Spiro compounds

ABSTRACT

Compounds of the formula (I): 
                         
(wherein
         A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom;   Ar 1  is aryl or heteroaryl, any of which is optionally substituted;   n is 0 or 1;   R 0  is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A;   T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group;   X is —N(SO 2 R 1 )—, —N(COR 2 )— or —CO—;   Y is —C(R 3 )(R 4 )—, —O— or —N(R 5 )—;   Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc., metabolic diseases such as obesity, diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia, etc., sexual and reproductive dysfunctions, and gastro-intestinal motility disorder.

This application is a U.S. national stage of International ApplicationNo. PCT/JP02/07922 filed Aug. 2, 2002.

TECHNICAL FIELD

The present invention is useful in medical fields. In more detail, spirocompounds of the present invention have an effect as neuropeptide Yreceptor antagonists and are useful as agents for the treatment ofvarious kinds of cardiovascular disorders, central nervous systemdisorders, metabolic diseases, and the like.

BACKGROUND ART

Neuropeptide Y (hereinafter referred to as NPY), a peptide consisting of36 amino acids, was first isolated from porcine brain by Tatemoto et alin 1982 (NATURE, vol. 296, p 659(1982)). NPY is widely distributed incentral nervous system and peripheral nervous system, and plays variousroles as one of the most abundant peptides in the nervous system. Thatis, npy acts as an orexigenic substance in the central nervous systemand markedly promotes fat accumulation via the mediation of secretion ofvarious hormones or the action of the nervous system. It is known thatcontinuous intracerebroventricular administration of NPY induces obesityand insulin resistance due to these actions (INTERNATIONAL JOURNAL OFOBESITY, vol. 19, p. 517(1995); Endocrinology, vol. 133, p. 1753(1993)).It is also known that NPY has central actions such as depression,anxiety, schizophrenia, pain, dementia, circadian rhythm control and thelike (DRUGS, vol. 52, p. 371(1996); THE JOURNAL OF NEUROSCIENCE, vol.18, p. 3014(1998)). Furthermore, in the periphery, NPY coexists withnorepinephrine in sympathetic-nerve terminals and is related to thetonicity of the sympathetic nervous system. It is known that peripheraladministration of NPY causes vasoconstriction and enhances theactivities of other vasoconstrictive substances such as norepinephrine(BRITISH JOURNAL OF PHARMACOLOGY, vol. 95, p. 419(1988)). It is alsoreported that NPY could participate in the development of cardiachypertrophy as a result of the sympathetic stimulation (PROCEEDINGS OFTHE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol.97, p. 1595(2000)).

On the other hand, it is reported that NPY is also involved in thesecretory function of sexual hormones and growth hormone, sexualbehavior and reproductive function, gastro-intestinal motility,bronchoconstriction, inflammation and alcohol preference (LIFE SCIENCE,vol. 55, p. 551(1994); THE JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY,vol. 101, p. S345(1998); NATURE, vol. 396, p. 366(1998)).

NPY has a variety of pharmacological effects resulting from NPY bindingto some NPY receptors to which peptide YY and pancreatic polypeptide,which are the analogs of NPY, also bind. It is known that thesepharmacological effects of NPY are mediated by the action of at leastfive receptors with or without synergistic interactions (TRENDS INNEUROSCIENCES, vol. 20, p. 294(1997)).

It is reported that the central effects mediated by NPY Y1 receptorinclude remarkable orexigenic effect (ENDOCRINOLOGY, vol. 137, p.3177(1996); ENDOCRINOLOGY, vol. 141, p. 1011(2000)). Further, NPY Y1receptor is reported to be involved in anxiety and pain (NATURE, vol.259, p. 528(1993); BRAIN RESEARCH, vol. 859, p. 361(2000). In addition,the pressor effect mediated by the strong vasoconstrictor action in theperiphery is also reported (FEBS LETTERS, vol. 362, p. 192(1995); NATUREMEDICINE, vol. 4, p. 722(1998)).

It is known that the effects mediated by NPY Y2 receptor include aninhibitory effect on the release of various neurotransmitters in thesympathetic nerve endings (BRITISH JOURNAL OF PHARMACOLOGY, vol. 102, p.41(1991); SYNAPSE, vol. 2, p. 299(1988)). In periphery, NPY Y2 causesconstriction of blood vessel or vas deferens directly or via the controlof release of various neurotransmitters (THE JOURNAL OF PHARMACOLOGY ANDEXPERIMENTAL THERAPEUTICS, vol. 261, p. 863(1992); BRITISH JOURNAL OFPHARMACOLOGY, vol. 100, p. 190(1990)). Inhibition of lipolysis inadipose tissues is also known (ENDOCRINOLOGY, vol. 131, p. 1970(1992)).Further, inhibition of ion secretion in the gastro-intestinal tract isreported (BRITISH JOURNAL OF PHARMACOLOGY, vol. 101, p. 247(1990)). Onthe other hand, the effects on the central nervous system functions suchas memory, anxiety and the like are also known (BRAIN RESEARCH, vol.503, p. 73(1989); PEPTIDES, vol. 19, p. 359(1998)).

It is reported that NPY Y3 receptor exists mainly in brainstem andheart, and is related to the regulation of blood pressure and heart rate(THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol. 258, p.633(1991); PEPTIDES, vol. 11, p. 545(1990)). It is also known that NPYY3 is involved in the control of catecholamine secretion in adrenalgland (THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, vol.244, p. 468(1988); LIFE SCIENCE, vol. 50, p. PL7(1992)).

NPY Y4 receptor has high affinity for pancreatic polypeptide inparticular. As for the pharmacological effects of NPY Y4, inhibition ofpancreatic exocrine secretion and gastro-intestinal motility is reported(GASTROENTEROLOGY, vol. 85, p. 1411(1983)). Further, it is reported thatNPY enhances the secretion of sexual hormones in the central nervoussystem (ENDOCRINOLOGY, vol. 140, p. 5171(1999)).

As for the effects mediated by NPY Y5 receptor, fat accumulation effectsincluding orexigenic effect are prominent (NATURE, vol. 382, p.168(1996); AMERICAN JOURNAL OF PHYSIOLOGY, vol. 277, p. R1428(1999)). Itis also reported that the NPY Y5 receptor mediates some CNS effects,such as seizure and epilepsy, or pain and morphine withdrawal symptoms,and the control of circadian rhythm (NATURE MEDICINE, vol. 3, p.761(1997); PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITEDSTATES OF AMERICA, vol. 96, p. 13518(1999); THE JOURNAL OF PHARMACOLOGYAND EXPERIMENTAL THERAPEUTICS, vol. 284, p. 633(1998); THE JOURNAL OFNEUROSCIENCE, vol. 21, p. 5367(2001). In addition, diuretic effect andhypoglicemic effect in the periphery are reported (BRITISH JOURNAL OFPHARMACOLOGY, vol. 120, p. 1335(1998); ENDOCRINOLOGY, vol. 139, p.3018(1998)). NPY is also reported to enhance cardiac hypertrophy as aresult of the sympathetic accentuation (PROCEEDINGS OF THE NATIONALACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol. 97, p. 1595(2000)).

The effects of NPY are expressed when NPY binds to the NPY receptors inthe central or peripheral nervous system. Therefore, the action of NPYcan be prevented by blocking its binding to NPY receptors. For thisreason, it is expected that substances antagonize NPY binding to NPYreceptors may be useful for the prophylaxis or treatment of variousdiseases related to NPY, for example, cardiovascular disorders such ashypertension, nephropathy, heart disease, vasospasm, etc., centralnervous system disorders such as bulimia, depression, anxiety, seizure,epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythmdisorders, schizophrenia, etc., metabolic diseases such as obesity,diabetes, hormone abnormality, etc., sexual and reproductivedysfunctions, gastro-intestinal motility disorders, respiratorydisorders, inflammatory diseases or glaucoma, and the like. (TRENDS INPHARMACOLOGICAL SCIENCES, vol. 15, p. 153(1994); LIFE SCIENCE, vol. 55,p. 551(1994); DRUGS, vol. 52, p. 371(1996); THE JOURNAL OF ALLERGY ANDCLINICAL IMMUNOLOGY, vol. 101, p. S345(1998); NATURE, vol. 396, p.366(1998); THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS,vol. 284, p. 633(1998); TRENDS IN PHARMACOLOGICAL SCIENCES, vol. 20, p.104(1999); PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITEDSTATES OF AMERICA, vol. 97, p. 1595(2000); THE JOURNAL OF NEUROSCIENCE,vol. 21, p. 5367(2001); PHARMACOLOGY & THERAPEUTICS, vol. 65, p.397(1995).

It was recently found that, as a result of the study by the presentinventors, certain NPY receptor antagonists are useful for theprophylaxis or treatment of hypercholesterolemia, hyperlipidemia andarteriosclerosis (International application publication WO99/27965).

DISCLOSURE OF THE INVENTION

The object of the present invention is to provide novel medicines whichhave NPY antagonistic actions.

The present inventors have discovered that compounds of the formula (I):

(wherein

A is a straight-chain hydrocarbon having 1 to 6 carbon atoms, which isoptionally substituted by a substituent selected from the groupconsisting of oxo, amino, lower alkylamino, di-lower alkylamino,hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl,heteroaryl and —R^(a), and is optionally intervened by oxygen ornitrogen atom;

Ar¹ is aryl or heteroaryl, any of which is optionally substituted by asubstituent selected from the group consisting of halogen, nitro, oxo,lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl,lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino,di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, loweralkoxycarbonyl and -Q-Ar²;

Ar² is aryl or heteroaryl, any of which is optionally substituted by asubstituent selected from the group consisting of halogen, cyano, loweralkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy,halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyland aryl;

n is 0 or 1;

Q is a single bond or carbonyl;

R^(a) is lower alkyl which is optionally substituted by a substituentselected from the group consisting of amino, lower alkylamino, di-loweralkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, thelast three groups being optionally substituted by fluorine;

R⁰ is hydrogen, or lower alkylene attached to an arbitrary, bondableposition of A;

R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl;

R³ and R⁴ are independently hydrogen, hydroxy, lower alkyl, aralkyl oraryl;

T, U, V and W are independently methine or nitrogen atom, said methinebeing optionally substituted by a substituent-selected from the groupconsisting of halogen, lower alkyl, hydroxy and lower alkoxy, and atleast two of T, U, V and W are said methine group;

X is —N(SO₂R¹)—, —N(COR²)— or —CO—;

Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—;

Z is methine or nitrogen atom)

exhibit NPY antagonistic activities and are useful as agents fortreatment of various kinds of diseases related to NPY, thereby completedthe present invention.

The compounds of the present invention (I) are useful as agents for thetreatment of various diseases related to NPY, that is, cardiovasculardisorders such as hypertension, nephropathy, heart disease, vasospasm,arteriosclerosis, etc., central nervous system disorders such asbulimia, depression, anxiety, seizure, epilepsy, dementia, pain,alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia,etc., metabolic diseases such as obesity, diabetes, hormone abnormality,hypercholesterolemia, hyperlipidemia, etc., sexual and reproductivedysfunctions, gastro-intestinal disorders such as gastro-intestinalmotility disorder, respiratory disorders, inflammatory diseases orglaucoma, and the like.

The compounds of the present invention (I) are particularly useful asagents for the treatment of bulimia, obesity, diabetes and the like.

The present invention relates to the compounds of the formula (I), orthe salts or esters thereof, and the production methods and the usethereof.

The means of terms used in the present specification are defined, andmore detailed description of this invention is described below.

“Halogen” refers to fluorine, chlorine, bromine and iodine.

“Lower alkyl” refers to a straight- or branched-chain alkyl group having1 to 6 carbon atoms, and its examples are methyl, ethyl, propyl,isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl,hexyl, isohexyl and the like.

“Halo-lower alkyl” refers to said lower alkyl substituted withidentically or differently one, two or more, preferably one to threesaid halogen at the arbitrary, substitutable position(s), and itsexamples are fluoromethyl, difluoromethyl, trifluoromethyl,2-fluoroethyl, 1,2-difluoroethyl, chloromethyl, 2-chloroethyl,1,2-dichloroethyl, bromomethyl, iodomethyl and the like.

“Hydroxy-lower alkyl” refers to said lower alkyl substituted with one,two or more, preferably one or two hydroxy at the arbitrary,substitutable position(s), and its examples are hydroxymethyl,2-hydroxyethyl, 1-hydroxy-1-methylethyl, 1,2-dihydroxyethyl,3-hydroxypropyl and the like.

“Cyclo-lower alkyl” refers to a cycloalkyl group having 3 to 6 carbonatoms, and its examples are cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl and the like.

“Lower alkenyl” refers to a straight- or branched-chain alkenyl grouphaving 2 to 6 carbon atoms, and its examples are vinyl, 1-propenyl,2-propenyl, isopropenyl, 3-butenyl, 2-butenyl, 1-butenyl,1-methyl-2-propenyl, 1-methyl-1-propenyl, 1-ethyl-1-ethenyl,2-methyl-2-propenyl, 2-methyl-1-propenyl, 3-methyl-2-butenyl, 4-pentenyland the like.

“Lower alkoxy” refers to a straight- or branched-chain alkoxy grouphaving 1 to 6 carbon atoms, and its examples are methoxy, ethoxy,propoxy, isopropoxy, butoxy, sec-butoxy, isobutoxy, tert-butoxy,pentyloxy, isopentyloxy, hexyloxy, isohexyloxy, and the like.

“Halo-lower alkoxy” refers to said lower alkoxy substituted withidentically or differently one, two or more, preferably one to threesaid halogen at the arbitrary, substitutable position(s), auditsexamples are fluoromethoxy, difluoromethoxy, trifluoromethoxy,2-fluoroethoxy, 1,2-difluoroethoxy, chloromethoxy, 2-chloroethoxy,1,2-dichloroethoxy, bromomethoxy, iodomethoxy and the like.

“Lower alkylthio” refers to a straight-or branched-chain alkylthio grouphaving 1 to 6 carbon atoms, and its examples are methylthio, ethylthio,propylthio, isopropylthio, butylthio, sec-butylthio, isobutylthio,tert-butylthio, pentylthio, isopentylthio, hexylthio, isohexylthio andthe like.

“Lower alkanoyl” refers to an alkanoyl group containing said loweralkyl, that is, an alkanoyl group having 2 to 7 carbon atoms, and itsexamples are acetyl, propionyl, butyryl, isobutyryl, valeryl,isovaleryl, pivaloyl and the like.

“Lower alkoxycarbonyl” refers to an alkoxycarbonyl group containing saidlower alkoxy, that is, an alkoxycarbonyl group having 2 to 7 carbonatoms, and its examples are methoxycarbonyl, ethoxycarbonyl,propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, isobutoxycarbonyl,tert-butoxycarbonyl, pentyloxycarbonyl and the like.

“Aryl” refers to phenyl, naphthyl and the like.

“Heteroaryl” refers to 5- or 6-membered monocyclic heteroaromatic groupwhich contains one, two or more, preferably one to three hetero atom(s)identically or differently selected from the group consisting of oxygen,nitrogen and sulfur; or condensed cyclic heteroaromatic group, wheresaid monocyclic heteroaromatic group is condensed with said aryl groupor condensed each other with the same or different said monocyclicheteroaromatic group, and its examples are pyrrolyl, furyl, thienyl,imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl,triazolyl, tetrazolyl, oxadiazolyl, 1,2,3-thiadiazolyl,1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, pyridyl, pyrazinyl, pyrimidinyl,pyridazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, indolyl, benzofuranyl,benzothienyl, benzoimidazolyl, benzoxazolyl, benzoisoxazolyl,benzothiazolyl, benzoisothiazolyl, indazolyl, purinyl, quinolyl,isoquinolyl, phthalazinyl, naphthylidinyl, quinoxalinyl, quinazolinyl,cinnolinyl, pteridinyl, pyrido[3,2-b]pyridyl and the like.

“A straight-chain hydrocarbon having 1 to 6 carbon atoms, which isoptionally intervened by oxygen or nitrogen atom” refers to a saturatedor unsaturated straight-chain hydrocarbon having 1 to 6 carbon atoms,which may or may not be intervened by one, two or more, preferably oneoxygen or nitrogen atom(s), at the arbitrary position(s) capable ofbeing intervened, and examples thereof are methylene, ethylene,trimethylene, tetramethylene, pentamethylene, 1-azatrimethylene,1-azatetramethylene, 2-azatetramethylene, 2-oxatetramethylene,2-oxapentamethylene, 3-oxapentamethylene and the like.

“Lower alkylamino” refers to an amino group mono-substituted with saidlower alkyl, and its examples are methylamino, ethylamino, propylamino,isopropylamino, butylamino, sec-butylamino, tert-butylamino and thelike.

“Di-lower alkylamino” refers to an amino group di-substituted withidentical or different said lower alkyl, and its examples aredimethylamino, diethylamino, ethylmethylamino, dipropylamino,methylpropylamino, diisopropylamino and the like.

“Lower alkylene” refers to a straight- or branched-chain alkylene grouphaving 1 to 6 carbon atoms, and its examples are methylene, ethylene,trimethylene, tetramethylene, pentamethylene, hexamethylene and thelike.

“Aralkyl” refers to said lower alkyl substituted with one, two or more,preferably one or two aryl at the arbitrary, substitutable position(s),and its examples are benzyl, 2-phenylethyl, 3-phenylethyl, 1-phenylethyland the like.

The salts of the compounds of the formula (I) refer to thepharmaceutically acceptable, common salts, and examples thereof are baseaddition salt to said carboxyl group when the compound has a carboxylgroup, or acid addition salt to an amino or said basic heterocyclyl whenthe compound has a basic heterocyclyl group, and the like.

Said base addition salts include salts with alkali metals (e.g. sodium,potassium); salts with alkaline earth metals (e.g. calcium, magnesium);ammonium salts; salts with organic amines (e.g. trimethylamine,triethylamine, dicyclohexylamine, ethanolamine, diethanolamine,triethanolamine, procaine, N,N′-dibenzylethylenediamine) and the like.

Said acid addition salts include salts with inorganic acids (e.g.hydrochloric acid, sulfuric acid, nitric acid, phosphoric acid,perchloric acid), salts with organic acids (e.g. maleic acid, fumaricacid, tartaric acid, citric acid, ascorbic acid, trifluoroacetic acid),salts with sulfonic acids (e.g. methanesulfonic acid, isethionic acid,benzenesulfonic acid, p-toluenesulfonic acid) and the like.

The esters of the compounds of the formula (I) refer to, for example,the pharmaceutically acceptable, common esters of said carboxyl groupwhen the compound has a carboxyl group, and examples thereof are esterswith lower alkyl (e.g. methyl, ethyl, propyl, isopropyl, butyl,sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, cyclopropyl,cyclobutyl, cyclopentyl), esters with aralkyl (e.g. benzyl, phenethyl),esters with lower alkenyl (e.g. allyl, 2-butenyl), esters withlower-alkoxy-lower-alkyl (e.g. methoxymethyl, 2-methoxyethyl,2-ethoxyethyl), esters with lower-alkanoyloxy-lower-alkyl (e.g.acetoxymethyl, pivaloyloxymethyl, 1-pivaloyloxyethyl), esters withlower-alkoxycarbonyl-lower-alkyl (e.g. methoxycarbonylmethyl,isopropoxycarbonylmethyl), esters with carboxy-lower alkyl (e.g.carboxymethyl), esters with lower-alkoxycarbonyloxy-lower-alkyl (e.g.1-(ethoxycarbonyloxy)ethyl, 1-(cyclohexyloxycarbonyloxy)ethyl), esterswith carbamoyloxy-lower alkyl (e.g. carbamoyloxymethyl), esters withphthalidyl, esters with (5-substituted-2-oxo-1,3-dioxol-4-yl)methyl(e.g. (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl) and the like.

“An agent for treatment” refers to a medicament which is employed forthe treatment and/or prophylaxis of various diseases.

In order to disclose the aforesaid compounds of the formula (I) of thepresent invention more specifically, the various symbols used in theformula (I) are explained in more detail by presenting preferredembodiments.

A refers to a straight-chain hydrocarbon having 1 to 6 carbon atoms,which is optionally substituted by a substituent selected from the groupconsisting of oxo, amino, lower alkylamino, di-lower alkylamino,hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl,heteroaryl and —R^(a), and is optionally intervened by oxygen ornitrogen atom.

“A straight-chain hydrocarbon having 1 to 6 carbon atoms, which isoptionally substituted by a substituent selected from the groupconsisting of oxo, amino, lower alkylamino, di-lower alkylamino,hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl,heteroaryl and —R^(a), and is optionally intervened by oxygen ornitrogen atom” refers to unsubstituted said straight-chain hydrocarbonhaving 1 to 6 carbon atoms, which is optionally intervened by oxygen ornitrogen atom; or said straight-chain hydrocarbon having 1 to 6 carbonatoms, which has substituent(s) at the arbitrary, substitutableposition(s), and is optionally intervened by oxygen or nitrogen atom,wherein said substituent may be one, two or more member(s), preferablyone member identically or differently selected from the group consistingof oxo, amino, lower alkylamino, di-lower alkylamino, hydroxy, loweralkoxy, lower alkoxycarbonyl, lower alkylene, aryl, heteroaryl and—R^(a).

The preferable examples of lower alkylamino as said substituent includemethylamino, ethylamino, propylamino and the like.

The preferable examples of di-lower alkylamino as said substituentinclude dimethylamino, diethylamino and the like.

The preferable examples of lower alkoxy as said substituent includemethoxy, ethoxy, propoxy and the like.

The preferable examples of lower alkoxycarbonyl as said substituentinclude methoxycarbonyl, ethoxycarbonyl and the like.

The preferable examples of lower alkylene as said substituent includemethylene, ethylene, trimethylene and the like.

The preferable examples of aryl as said substituent include phenyl,naphthyl and the like.

The preferable examples of heteroaryl as said substituent includepyridyl, quinolyl, indolyl and the like.

A group represented by the formula: —R^(a) as said substituent refers tolower alkyl which is optionally substituted by a substituent selectedfrom the group consisting of amino, lower alkylamino, di-loweralkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, thelast three groups being optionally substituted by fluorine.

“Lower alkyl which is optionally substituted by a substituent selectedfrom the group consisting of amino, lower alkylamino, di-loweralkylamino and hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, thelast three groups being optionally substituted by fluorine” refers tounsubstituted said lower alkyl, or said lower alkyl havingsubstituent(s) at the arbitrary, substitutable position(s), wherein saidsubstituent may be one, two or more, preferably one member(s)identically or differently selected from the group consisting of amino,lower alkylamino, di-lower alkylamino and hydroxy, and cyclo-loweralkyl, aryl and heteroaryl, the last three groups being optionallysubstituted by fluorine.

The preferable examples of lower alkylamino as said substituent includemethylamino, ethylamino, propylamino and the like.

The preferable examples of di-lower alkylamino as said substituentinclude dimethylamino, diethylamino and the like.

The preferable examples of cyclo-lower alkyl being optionallysubstituted by fluorine as said substituent include cyclopentyl,cyclohexyl and the like.

The preferable examples of aryl being optionally substituted by fluorineas said substituent include phenyl, 4-fluorophenyl, naphthyl and thelike.

The preferable examples of heteroaryl being optionally substituted byfluorine as said substituent include pyridyl, quinolyl, indolyl and thelike.

The preferable examples of lower alkyl of “lower alkyl which isoptionally substituted” as R^(a) include methyl, ethyl, propyl and thelike.

The preferable examples of R^(a) include hydroxymethyl,cyclohexylmethyl, benzyl, 4-fluorobenzyl, 3-pyridylmethyl,4-pyridylmethyl, 3-indolylmethyl and the like.

The preferable examples of substituent of A include oxo, hydroxy, loweralkoxycarbonyl, lower alkylene, aryl, —R^(a) and the like.

To be more specific, A includes, for example, a group of the formula(A-1) and (A-2):

and the like.

Ar¹ is aryl or heteroaryl, any of which is optionally substituted by asubstituent selected from the group consisting of halogen, nitro, oxo,lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl,lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino,di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, loweralkoxycarbonyl and -Q-Ar².

“Aryl or heteroaryl, any of which is optionally substituted by asubstituent selected from the group consisting of halogen, nitro, oxo,lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl,lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino,di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, loweralkoxycarbonyl and -Q-Ar²” refers to unsubstituted said aryl or saidheteroaryl, or said aryl or said heteroaryl, the last two groups havingsubstituent(s) at the arbitrary, substitutable position(s) wherein saidsubstituent may be one, two or more, preferably one or two member(s)identically or differently selected from the group consisting ofhalogen, nitro, oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl,cyclo-lower alkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, loweralkylamino, di-lower alkylamino, lower alkylthio, carboxyl, loweralkanoyl, lower alkoxycarbonyl and -Q-Ar².

The preferable examples of halogen as said substituent include fluorine,chlorine and the like.

The preferable examples of lower alkyl as said substituent includemethyl, ethyl, propyl, isopropyl and the like.

The preferable examples of halo-lower alkyl as said substituent includedifluoromethyl, trifluoromethyl and the like.

The preferable examples of hydroxy-lower alkyl as said substituentinclude hydroxymethyl, 2-hydroxyethyl, 1-hydroxy-methylethyl and thelike.

The preferable examples of cyclo-lower alkyl as said substituent includecyclopropyl, cyclobutyl and the like.

The preferable examples of lower alkenyl as said substituent includevinyl, 1-propenyl, 2-methyl-1-propenyl and the like.

The preferable examples of lower alkoxy as said substituent includemethoxy, ethoxy and the like

The preferable examples of halo-lower alkoxy as said substituent includefluoromethoxy, difluoromethoxy, trifluoromethoxy and the like.

The preferable examples of lower alkylamino as said substituent includemethylamino, ethylamino, propylamino and the like.

The preferable examples of di-lower alkylamino as said substituentinclude dimethylamino, diethylamino and the like.

The preferable examples of lower alkylthio as said substituent includemethylthio, ethylthio and the like.

The preferable examples of lower alkanoyl as said substituent includeacethyl, propionyl and the like.

The preferable examples of lower alkoxycarbonyl as said substituentinclude methoxycarbonyl, ethoxycarbonyl and the like.

In a group represented by the formula: -Q-Ar² as said substituent, Ar²is aryl or heteroaryl, any of which is optionally substituted by asubstituent selected from the group consisting of halogen, cyano, loweralkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy,halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyland aryl; Q is a single bond or carbonyl.

“Aryl or heteroaryl, any of which is optionally substituted by asubstituent selected from the group consisting of halogen, cyano, loweralkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy,halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyland aryl” refers to unsubstituted said aryl or said heteroaryl, or saidaryl or said heteroaryl, the last two groups having substituent(s) atthe arbitrary, substitutable position(s) wherein said substituent may beone, two or more, preferably one or two member(s) identically ordifferently selected from the group consisting of halogen, cyano, loweralkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy, lower alkoxy,halo-lower alkoxy, lower alkylamino, di-lower alkylamino, lower alkanoyland aryl.

The preferable examples of halogen as said substituent include fluorine,chlorine and the like.

The preferable examples of lower alkyl as said substituent includemethyl, ethyl, propyl, isopropyl and the like.

The preferable examples of halo-lower alkyl as said substituent includedifluoromethyl, trifluoromethyl and the like.

The preferable examples of hydroxy-lower alkyl as said substituentinclude hydroxymethyl, 2-hydroxyethyl, 1-hydroxy-1-methylethyl and thelike.

The preferable examples of lower alkoxy as said substituent includemethoxy, ethoxy and the like.

The preferable examples of halo-lower alkoxy as said substituent includefluoromethoxy, difluoromethoxy, trifluoromethoxy and the like.

The preferable examples of lower alkylamino as said substituent includemethylamino, ethylamino and the like.

The preferable examples of di-lower alkylamino as said substituentinclude dimethylamino, diethylamino and the like.

The preferable examples of lower alkanoyl as said substituent includeacetyl, propionyl and the like.

The preferable examples of aryl as said substituent include phenyl andthe like.

The preferable examples of the substituent of Ar² include halogen,cyano, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, hydroxy,halo-lower alkoxy and the like.

The preferable examples of aryl as Ar² include phenyl and the like, andpreferred examples of heteroaryl as Ar² include imidazolyl, pyridyl,benzofuranyl, quinolyl and the like.

Thus, the preferable examples of a group represented by the formula:-Q-Ar² include phenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl,2,3-difluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl,2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2-cyanophenyl,3-cyanophenyl, 4-cyanophenyl, 2-methylphenyl, 3-methylphenyl,4-methylphenyl, 2-fluoro-5-methylphenyl, 3-fluoromethylphenyl,2-trifluoromethylphenyl, 3-trifluoromethylphenyl,4-trifluoromethylphenyl, 2-methoxyphenyl, 3-methoxyphenyl,4-methoxyphenyl, 3-fluoro-5-methoxyphenyl, 3-fluoromethoxyphenyl,3-difluoromethoxyphenyl, 3-(2-hydroxyethyl)phenyl,3-hydroxymethylphenyl, 3-(1-hydroxy-1-methylethyl)phenyl,3-hydroxyphenyl, 4-hydroxyphenyl, 2-imidazolyl, 1-ethyl-2-imidazolyl,1,2,4-thiadiazol-5-yl, 1,3,4-thiadiazol-2-yl, 2-pyridyl, 3-pyridyl,4-pyridyl, 2-ethyl-4-pyridyl, 4-pyrimidinyl, 5-pyrimidinyl,4-benzo[b]furanyl, 5-benzo[b]furanyl, 7-benzo[b]furanyl, 2-quinolyl,3-quinolyl, 4-quinolyl, 5-quinolyl, 6-quinolyl, 8-quinolyl, benzoyl,2-pyridylcarbonyl and the like, among which the more preferable examplesare phenyl, 2-fluorophenyl, 3-fluorophenyl, 3,5-difluorophenyl,3-chlorophenyl, 4-chlorophenyl, 3-cyanophenyl, 3-trifluoromethylphenyl,3-difluoromethoxyphenyl, 3-(2-hydroxyethyl)phenyl, 3-hydroxyphenyl,4-hydroxyphenyl, 1-ethyl-2-imidazolyl, 2-pyridyl, 7-benzo[b]furanyl,2-quinolyl, 3-quinolyl, benzoyl, 2-pyridylcarbonyl and the like.

The preferable examples of the substituent of Ar¹ include halogen, loweralkyl, halo-lower alkyl, lower alkenyl, lower alkoxy, di-loweralkylamino, lower alkanoyl, -Q-Ar² and the like, more preferably,halogen, halo-lower alkyl, lower alkoxy, di-lower alkylamino and thelike.

The preferable examples of aryl as Ar¹ preferably include phenyl and thelike, and the preferable examples of heteroaryl as Ar¹ preferablyinclude imidazolyl, pyrazolyl, thiazolyl, oxazolyl, isoxazolyl,1,2,4-thiadiazolyl, pyridyl, pyrazinyl, pyrimidinyl, 1,2,4-triazinyl,benzoxazolyl, benzothiazolyl, quinolyl, pyrido[3,2-b]pyridyl and thelike, more preferably, pyridyl and the like.

R⁰ refers to hydrogen, or lower alkylene attached to an arbitrary,bondable position of A.

The preferable examples of lower alkylene as R⁰ include methylene,ethylene, trimethylene, tetramethylene and the like.

Thus, a group represented by the formula: -A-Ar¹—R⁰ includes, forexample, 1-phenyl-3-pyrrolidinyl, 1-(2-fluorophenyl)-3-pyrrolidinyl,1-(3-fluorophenyl)-3-pyrrolidinyl, 1-(4-fluorophenyl)-3-pyrrolidinyl,1-(2-pyridyl)-3-pyrrolidinyl, 1-(3-pyridyl)-3-pyrrolidinyl,1-(4-pyridyl)-3-pyrrolidinyl, 1-(3,5-difluorophenyl)-3-pyrrolidinyl,1-(3-trifluoromethylphenyl)-3-pyrrolidinyl,1-(2-pyrimidinyl)-3-pyrrolidinyl, 5-oxo-1-phenyl-3-pyrrolidinyl,1-phenyl-4-piperidyl, 1-(2-fluorophenyl)-4-piperidyl,1-(3-fluorophenyl)-4-piperidyl, 1-(4-fluorophenyl)-4-piperidyl,1-(3,5-difluorophenyl)-4-piperidyl, 1-(2-pyridyl)-4-piperidyl,1-(3-pyridyl)-4-piperidyl, 1-(4-pyridyl)-4-piperidyl,3-hydroxymethyl-1-phenyl-4-piperidyl,3-methoxycarbonyl-1-phenyl-4-piperidyl,3-ethoxycarbonyl-1-phenyl-4-piperidyl,3-isopropoxycarbonyl-1-phenyl-4-piperidyl, 1-phenyl-3-piperidyl,1-(2-fluorophenyl)-3-piperidyl, 1-(3-fluorophenyl)-3-piperidyl,1-(4-fluorophenyl)-3-piperidyl, 1-(3,5-difluorophenyl)-3-piperidyl,1-(2-pyridyl)-3-piperidyl, 1-(3-pyridyl)-3-piperidyl,1-(4-pyridyl)-3-piperidyl, 3-phenylcyclopentyl, 3-phenylcyclohexyl,4-phenylcyclohexyl, 4-(2-fluorophenyl)cyclohexyl,4-(3-fluorophenyl)cyclohexyl, 4-(4-fluorophenyl)cyclohexyl,4-(2-pyridyl)cyclohexyl, 4-(3-pyridyl)cyclohexyl,4-(4-pyridyl)cyclohexyl, 4-(4-fluoro-3-pyridyl)cyclohexyl,4-(3-quinolyl)cyclohexyl, 4-(3-fluorophenyl)-4-hydroxycyclohexyl,6-phenyl-3-tetrahydropyranyl, 6-(3-fluorophenyl)-3-tetrahydropyranyl,2-phenylcyclopropyl, 2-(2-pyridyl)cyclopropyl, 2-(3-pyridyl)cyclopropyl,2-(4-pyridyl)cyclopropyl, 2-indanyl, 2-tetrahydronaphthyl,6-methoxy-2-tetrahydronaphthyl, benzyl, phenethyl, 3-phenylpropyl,4-phenylbutyl, 4-bromophenethyl, 3-methoxyphenethyl,2-propyloxyphenethyl, 4-dimethylaminophenethyl, 3,5-difluorophenethyl,3,4-dimethoxyphenethyl, 4-(dimethylamino)-2-methoxyphenethyl,2-(3-quinolyl)ethyl, 2-hydroxy-2-(3-quinolyl)ethyl,2-hydroxy-2-phenylethyl, benzoylmethyl,2-hydroxy-2-(4-dimethylaminophenyl)ethyl,2-hydroxy-2-(3,5-difluorophenyl)ethyl, 1-(hydroxymethyl)-2-phenylethyl,1-(methoxycarbonyl)-2-phenylethyl, 1-(aminomethyl)-2-phenylethyl,1-(isobutylaminomethyl)-2-phenylethyl, 1-benzyl-2-(benzylamino)ethyl,1-benzyl-2-anilinoethyl, 1-benzyl-2-(2-pyridylmethylamino)ethyl,1-benzyl-2-(3-pyridylmethylamino)ethyl,1-benzyl-2-(N-benzyl-N-methylamino)ethyl, 1-benzyl-2-(benzyloxy)ethyl,1-(cyclohexylmethyl)-2-(benzyloxy)ethyl,1-benzyloxycarbonyl-2-cyclohexylethyl,1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl,1-(benzylcarbamoyl)-2-phenylethyl,1-(benzylcarbamoyl)-2-cyclohexylethyl,1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl,1-(4-pyridylmethylcarbamoyl)-2-(4-fluorophenyl)ethyl,1-(N-methylbenzylcarbamoyl)-2-phenylethyl,1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl and the like, among whichthe more preferable examples are 1-phenyl-3-pyrrolidinyl,1-(2-fluorophenyl)-3-pyrrolidinyl, 1-(3-fluorophenyl)-3-pyrrolidinyl,1-(4-fluorophenyl)-3-pyrrolidinyl, 1-phenyl-4-piperidyl,1-(2-fluorophenyl)-4-piperidyl, 1-(3-fluorophenyl)-4-piperidyl,1-(3,5-difluorophenyl)-4-piperidyl, 4-phenylcyclohexyl,4-(2-fluorophenyl)cyclohexyl, 4-(3-fluorophenyl)cyclohexyl,4-dimethylaminophenethyl, 1-benzyl-2-(benzylamino)ethyl,1-benzyl-2-(2-pyridylmethylamino)ethyl,1-benzyl-2-(3-pyridylmethylamino)ethyl, 1-benzyl-2-(benzyloxy)ethyl,1-(benzylcarbamoyl)-2-phenylethyl,1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl and the like.

n is 0 or 1, preferably 0.

T, U, V and W are independently methine or nitrogen atom, said methanebeing optionally substituted by a substituent selected from the groupconsisting of halogen, lower alkyl, hydroxy and lower alkoxy, and atleast two of T, U, V and W are said methine group;

“Methine being optionally substituted by a substituent selected from thegroup consisting of halogen, lower alkyl, hydroxy and lower alkoxy”refers to unsubstituted methine or methine having a substituent selectedfrom the group consisting of halogen, lower alkyl, hydroxy and loweralkoxy.

The preferable examples of halogen as said substituent include fluorine,chlorine and the like.

The preferable examples of lower alkyl as said substituent includemethyl, ethyl and the like.

The preferable examples of lower alkoxy as said substituent includemethoxy, ethoxy and the like.

The preferable examples of the said substituent include halogen atom andthe like.

The preferred embodiments of T, U, V and W include the case where T, U,V and W are independently methine optionally having said substituent,preferably halogen; or the case where one of T, U, V and W is nitrogenatom; and the like.

X is —N(SO₂R¹)—, —N(COR²)— or —CO—;

Y is —C(R³)(R⁴)—, —O— or —N(R⁵)—;

R¹, R² and R⁵ are independently hydrogen, lower alkyl, aralkyl or aryl;

R³ and R⁴ are independently hydrogen, hydroxy, lower alkyl, aralkyl oraryl.

The preferable examples of lower alkyl as R¹, R², R³, R⁴ or R⁵ includeeach independently methyl, ethyl, propyl and the like.

The preferable examples of aralkyl as R¹, R², R³, R⁴ or R⁵ include eachindependently benzyl and the like.

The preferable examples of aryl as R¹, R², R³, R⁴ or R⁵ include eachindependently phenyl and the like.

The preferable examples of R¹ and R² include lower alkyl and the like.

The preferred embodiments of R³ and R⁴ are the case where both R³ and R⁴are hydrogen, and the like.

The preferable examples of R⁵ include hydrogen, lower alkyl and thelike, more preferably hydrogen and the like.

The preferred embodiment of X, Y and n includes, for example, the casewhere X is —N(SO₂R¹)— or —N(COR²)—, preferably —N(SO₂R¹)—, n is 0, and Yis —C(R³)(R⁴)—; or the case where X is —CO—, and Y is —O— or —N(R⁵)—,more preferably —O—, and among which the case where X is —CO— and Y is—O— or —NH—; and the case where X is —CO— and Y is —O— are morepreferable.

Z is methine or nitrogen atom, preferably methine.

In more detail, the preferable examples of a group of the formula (VII):

include a group represented by the following formulas (VIII):

(wherein R¹ has the same meaning as defined above) and the like.

Preferred compounds of the formula (I) are, for example, compounds ofthe formula (I-a):

wherein A, Ar¹, R⁰ and R¹ have the same meaning as defined above,compounds of the formula (I-b):

wherein A, Ar¹, R⁰ and R¹ have the same meaning as defined above,compounds of the formula (I-c):

wherein A, Ar¹ and R⁰ have the same meaning as defined above, compoundsof the formula (I-d):

wherein A, Ar¹, R⁰, T, U, V and W have the same meaning as definedabove, and compounds of the formula (I-e):

wherein A, Ar¹ and R⁰ have the same meaning as defined above.

Preferred compounds of the formula (I-d) are, for example, compoundswherein all of T, U, V and W are unsubstituted methine, or compoundswherein one of T, U, V and W is nitrogen atom.

Preferred compounds of the formula (I), (I-a), (I-b), (I-c), (I-d) or(I-e) are, for example, compounds wherein aryl as Ar¹ is phenyl, orcompounds wherein Ar¹ is heteroaryl which is optionally substituted by asubstituent selected from the group consisting of halogen, nitro, oxo,lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl,lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino,di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl, loweralkoxycarbonyl and -Q-Ar².

The compounds of the present invention may include stereoisomers such asoptical isomers, diastereoisomers and geometrical isomers, or tautomersdepending upon the mode of substituents. The compounds of the presentinvention include all the stereoisomers, tautomers and their mixtures.

For example, compounds of the formula (I-b) include stereoisomers suchas trans-form compound of the formula (I-1b):

and cis-form compound of the formula (I-2b):

among which trans-form compound is preferred.

Also, compounds of the formula (I-d) include stereoisomers such astrans-form compound of the formula (I-1d):

and cis-form compound of the formula (I-2d):

among which trans-form compound is preferred.

Also included within the scope of the invention are polymorphs, hydratesand solvates of the compounds of the present invention.

The present invention also includes prodrugs of the compounds of thepresent invention within its scope. In general, such prodrugs arefunctional derivatives of the compounds of the present invention whichcan be readily converted in vivo into the required compound. Thus, inthe treatment methods for various diseases according to the presentinvention, the term “administering” shall encompass not onlyadministration of the compound specified in this disclosure but alsoadministration of a compound which is converted in vivo into thespecified compound when it is administered to a patient. Conventionalprocedures for selection and preparation of suitable prodrug derivativesare described, for example, in “Design of Prodrugs,” ed. H. Bundgaard,Elsevier (1985), which are referred and entirely incorporated in thisspecification. The metabolites of these compounds include activecompounds which are produced upon introduction of compounds of thepresent invention into the biological milieu, and they are encompassedin the scope of the present invention.

The specific compounds of the formula (I) are, for example, followingcompounds.

In the tables, Me refers to methyl group, and Et refers to ethyl group.

TABLE 1

No. R¹ Z A—Ar¹—R⁰ 1 Me CH 1-phenyl-3-pyrrolidinyl 2 Me CH1-(2-fluorophenyl)-3-pyrrolidinyl 3 Me CH1-(3-fluorophenyl)-3-pyrrolidinyl 4 Me CH1-(4-fluorophenyl)-3-pyrrolidinyl 5 Me CH1-(2-chlorophenyl)-3-pyrrolidinyl 6 Me CH1-(3-chlorophenyl)-3-pyrrolidinyl 7 Me CH1-(4-chlorophenyl)-3-pyrrolidinyl 8 Me CH1-(2-methylphenyl)-3-pyrrolidinyl 9 Me CH1-(3-methylphenyl)-3-pyrrolidinyl 10 Me CH1-(4-methylphenyl)-3-pyrrolidinyl 11 Me CH1-(2-methoxyphenyl)-3-pyrrolidinyl 12 Me CH1-(3-methoxyphenyl)-3-pyrrolidinyl 13 Me CH1-(4-methoxyphenyl)-3-pyrrolidinyl 14 Me CH1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 15 Me CH1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 16 Me CH1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 17 Me CH1-(3,5-difluorophenyl)-3-pyrrolidinyl 18 Me CH1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 19 Me CH1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 20 Me CH1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 21 Me CH1-(2-pyridyl)-3-pyrrolidinyl 22 Me CH 1-(3-pyridyl)-3-pyrrolidinyl 23 MeCH 1-(4-pyridyl)-3-pyrrolidinyl 24 Me CH1-(2-pyrimidinyl)-3-pyrrolidinyl 25 Me CH 5-oxo-1-phenyl-3-pyrrolidinyl26 Me CH 1-phenyl-3-piperidyl 27 Me CH 1-(2-fluorophenyl)-3-piperidyl 28Me CH 1-(3-fluorophenyl)-3-piperidyl 29 Me CH1-(4-fluorophenyl)-3-piperidyl 30 Me CH 1-(2-chlorophenyl)-3-piperidyl31 Me CH 1-(3-chlorophenyl)-3-piperidyl 32 Me CH1-(4-chlorophenyl)-3-piperidyl 33 Me CH 1-(2-methylphenyl)-3-piperidyl34 Me CH 1-(3-methylphenyl)-3-piperidyl 35 Me CH1-(4-methylphenyl)-3-piperidyl 36 Me CH 1-(2-methoxyphenyl)-3-piperidyl37 Me CH 1-(3-methoxyphenyl)-3-piperidyl 38 Me CH1-(4-methoxyphenyl)-3-piperidyl 39 Me CH1-(2-trifluoromethylphenyl)-3-piperidyl 40 Me CH1-(3-trifluoromethylphenyl)-3-piperidyl 41 Me CH1-(4-trifluoromethylphenyl)-3-piperidyl 42 Me CH1-(3,5-difluorophenyl)-3-piperidyl 43 Me CH1-(2-difluoromethoxyphenyl)-3-piperidyl 44 Me CH1-(3-difluoromethoxyphenyl)-3-piperidyl 45 Me CH1-(4-difluoromethoxyphenyl)-3-piperidyl 46 Me CH1-(2-pyridyl)-3-piperidyl 47 Me CH 1-(3-pyridyl)-3-piperidyl 48 Me CH1-(4-pyridyl)-3-piperidyl 49 Me CH 1-phenyl-4-piperidyl 50 Me CH1-(2-fluorophenyl)-4-piperidyl 51 Me CH 1-(3-fluorophenyl)-4-piperidyl52 Me CH 1-(4-fluorophenyl)-4-piperidyl 53 Me CH1-(2-chlorophenyl)-4-piperidyl 54 Me CH 1-(3-chlorophenyl)-4-piperidyl55 Me CH 1-(4-chlorophenyl)-4-piperidyl 56 Me CH1-(2-methylphenyl)-4-piperidyl 57 Me CH 1-(3-methylphenyl)-4-piperidyl58 Me CH 1-(4-methylphenyl)-4-piperidyl 59 Me CH1-(2-methoxyphenyl)-4-piperidyl 60 Me CH 1-(3-methoxyphenyl)-4-piperidyl61 Me CH 1-(4-methoxyphenyl)-4-piperidyl 62 Me CH1-(2-trifluoromethylphenyl)-4-piperidyl 63 Me CH1-(3-trifluoromethylphenyl)-4-piperidyl 64 Me CH1-(4-trifluoromethylphenyl)-4-piperidyl 65 Me CH1-(3,5-difluorophenyl)-4-piperidyl 66 Me CH1-(2-difluoromethoxyphenyl)-4-piperidyl 67 Me CH1-(3-difluoromethoxyphenyl)-4-piperidyl 68 Me CH1-(4-difluoromethoxyphenyl)-4-piperidyl 69 Me CH1-(2-pyridyl)-4-piperidyl 70 Me CH 1-(3-pyridyl)-4-piperidyl 71 Me CH1-(4-pyridyl)-4-piperidyl 72 Me CH 3-hydroxymethyl-1-phenyl-4-piperidyl73 Me CH 3-methoxycarbonyl-1-phenyl-4-piperidyl 74 Me CH3-ethoxycarbonyl-1-phenyl-4-piperidyl 75 Me CH3-isopropoxycarbonyl-1-phenyl-4-piperidyl 76 Me CH 4-phenylcyclohexyl 77Me CH 4-(2-fluorophenyl)cyclohexyl 78 Me CH 4-(3-fluorophenyl)cyclohexyl79 Me CH 4-(4-fluorophenyl)cyclohexyl 80 Me CH4-(2-chlorophenyl)cyclohexyl 81 Me CH 4-(3-chlorophenyl)cyclohexyl 82 MeCH 4-(4-chlorophenyl)cyclohexyl 83 Me CH 4-(2-methylphenyl)cyclohexyl 84Me CH 4-(3-methylphenyl)cyclohexyl 85 Me CH 4-(4-methylphenyl)cyclohexyl86 Me CH 4-(2-methoxyphenyl)cyclohexyl 87 Me CH4-(3-methoxyphenyl)cyclohexyl 88 Me CH 4-(4-methoxyphenyl)cyclohexyl 89Me CH 4-(2-trifluoromethylphenyl)cyclohexyl 90 Me CH4-(3-trifluoromethylphenyl)cyclohexyl 91 Me CH4-(4-trifluoromethylphenyl)cyclohexyl 92 Me CH4-(3,5-difluorophenyl)cyclohexyl 93 Me CH 4-(3-acetylphenyl)cyclohexyl94 Me CH 4-(3-cyanophenyl)cyclohexyl 95 Me CH4-(2-difluoromethoxyphenyl)cyclohexyl 96 Me CH4-(3-difluoromethoxyphenyl)cyclohexyl 97 Me CH4-(4-difluoromethoxyphenyl)cyclohexyl 98 Me CH 4-(2-pyridyl)cyclohexyl99 Me CH 4-(3-pyridyl)cyclohexyl 100 Me CH 4-(4-pyridyl)cyclohexyl 101Me CH 4-(4-fluoro-3-pyridyl)cyclohexyl 102 Me CH4-(3-quinolyl)cyclohexyl 103 Me CH4-(3-fluorophenyl)-4-hydroxycyclohexyl 104 Me CH 3-phenylcyclohexyl 105Me CH 3-phenylcyclopentyl 106 Me CH 6-phenyl-3-tetrahydropyranyl 107 MeCH 6-(3-fluorophenyl)-3-tetrahydropyranyl 108 Me CH 2-phenylcyclopropyl109 Me CH 2-(2-pyridyl)cyclopropyl 110 Me CH 2-(3-pyridyl)cyclopropyl111 Me CH 2-(4-pyridyl)cyclopropyl 112 Me CH2-(3-fluorophenyl)cyclopropyl 113 Me CH 2-indanyl 114 Me CH2-tetrahydronaphthyl 115 Me CH 6-methoxy-2-tetrahydronaphthyl 116 Me CHbenzyl 117 Me CH phenethyl 118 Me CH 3-phenylpropyl 119 Me CH4-phenylbutyl 120 Me CH 2-methoxyphenethyl 121 Me CH 3-methoxyphenethyl122 Me CH 4-methoxyphenethyl 123 Me CH 4-fluorophenethyl 124 Me CH4-bromophenethyl 125 Me CH 4-chlorophenethyl 126 Me CH3-trifluoromethylphenethyl 127 Me CH 3,4-dimethoxyphenethyl 128 Me CH3-propoxyphenethyl 129 Me CH 3,5-difluorophenethyl 130 Me CH4-dimethylaminophenethyl 131 Me CH 3-difluoromethoxyphenethyl 132 Me CH2-methylphenethyl 133 Me CH 4-acetylphenethyl 134 Me CH4-dimethylamino-2-methoxyphenethyl 135 Me CH cyclohexylethyl 136 Me CH2-(2-pyridyl)ethyl 137 Me CH 2-(3-pyridyl)ethyl 138 Me CH2-(4-pyridyl)ethyl 139 Me CH 2-(2-quinolyl)ethyl 140 Me CH2-(3-quinolyl)ethyl l41 Me CH 2-(4-quinolyl)ethyl 142 Me CH2-(6-quinolyl)ethyl 143 Me CH 2-(2-indolyl)ethyl 144 Me CH2-(3-indolyl)ethyl 145 Me CH 2-(7-aza-3-indolyl)ethyl 146 Me CH2-(benzimidazolyl)ethyl 147 Me CH 2-(benzoxazolyl)ethyl 148 Me CH2-(benzothiazolyl)ethyl 149 Me CH 2-(1-naphthyl)ethyl 150 Me CH2-(2-naphthyl)ethyl 151 Me CH 1-(hydroxymethyl)-2-phenylethyl 152 Me CH1-(methoxycarbonyl)-2-phenylethyl 153 Me CH1-(ethoxycarbonyl)-2-phenylethyl 154 Me CH 1-carboxy-2-phenylethyl 155Me CH 1-(benzyloxycarbonyl)-2-phenylethyl 156 Me CH1-(phenoxymethyl)-2-phenylethyl 157 Me CH1-(benzyloxymethyl)-2-phenylethyl 158 Me CH1-(benzylcarbamoyl)-2-phenylethyl 159 Me CH1-(N-methylbenzylcarbamoyl)-2-phenylethyl 160 Me CH1-(phenylcarbamoyl)-2-phenylethyl 161 Me CH1-(M-methylphenylcarbamoyl)-2-phenylethyl 162 Me CH1-(N-benzylaminomethyl)-2-phenylethyl 163 Me CH1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 164 Me CH1-(anilinomethyl)-2-phenylethyl 165 Me CH1-(N-methylanilinomethyl)-2-phenylethyl 166 Me CH1-(N-methylaminomethyl)-2-phenylethyl 167 Me CH1-(N-ethylaminomethyl)-2-phenylethyl 168 Me CH1-(N-isobutylaminomethyl)-2-phenylethyl 169 Me CH1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 170 Me CH1-(aminomethyl)-2-phenylethyl 171 Me CH1-benzyl-2-(2-pyridylmethylamino)ethyl 172 Me CH1-benzyl-2-(3-pyridylmethylamino)ethyl 173 Me CH1-benzyl-2-(4-pyridylmethylamino)ethyl 174 Me CH2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 175 Me CH2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 176 Me CH2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 177 Me CH2-hydroxy-2-phenylethyl 178 Me CH benzoylmethyl 179 Me CH1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 180 Me CH1-(benzyloxycarbonyl)-2-cyclohexylethyl 181 Me CH1-(phenoxymethyl)-2-(3-indolyl)ethyl 182 Me CH 2-(2-methoxyphenoxy)ethyl183 Me CH 1-(benzylcarbamoyl)-2-cyclohexylethyl 184 Me CH1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 185 Me CH1-(phenylcarbamoyl)-2-cyclohexylethyl 186 Me CH1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 187 Me CH1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 188 Me CH1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 189 Me CH1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 190 Me CH1-(4-pyridylmethylcarbamoyl)-2-(4-fluoro- phenyl) ethyl 191 Me CH1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 192 Me CH1-(benzyloxymethyl)-2-(2-indolyl)ethyl 193 Me CH1-(N-benzyl-N-methylaminomethyl)-2-(3- pyridyl)ethyl 194 Me CH1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 195 Me CH2-hydroxy-2-(4-dimethylaminophenyl)ethyl 196 Me CH2-hydroxy-2-(2-quinolyl)ethyl 197 Me CH 2-hydroxy-2-(3-quinolyl)ethyl198 Me CH 2-hydroxy-2-(4-quinolyl)ethyl 199 Me CH2-hydroxy-2-(3,5-difluorophenyl)ethyl 200 Me CH1-carboxy-2-cyclohexylethyl 201 Me CH 2-hydroxy-2-(6-quinolyl)ethyl 202Me CH 2-(benzylamino)-2-phenylethyl 203 Me CH2-amino-2-(2-naphthyl)propyl 204 Me CH 2-(phenylamino)ethyl 205 Me CHdiphenylmethyl 206 Me CH 2,2-diphenylethyl 207 Me CH2-phenyl-2-(2-pyridyl)ethyl 208 Me CH 2-phenyl-2-(3-pyridyl)ethyl 209 MeCH 2-phenyl-2-(4-pyridyl)ethyl 210 Me CH 2-phenoxy-2-phenylethyl 211 MeCH 2-(benzyloxy)-2-phenylethyl 212 Et CH 1-phenyl-3-pyrrolidinyl 213 EtCH 1-(2-fluorophenyl)-3-pyrrolidinyl 214 Et CH1-(3-fluorophenyl)-3-pyrrolidinyl 215 Et CH1-(4-fluorophenyl)-3-pyrrolidinyl 216 Et CH1-(2-chlorophenyl)-3-pyrrolidinyl 217 Et CH1-(3-chlorophenyl)-3-pyrrolidinyl 218 Et CH1-(4-chlorophenyl)-3-pyrrolidinyl 219 Et CH1-(2-methylphenyl)-3-pyrrolidinyl 220 Et CH1-(3-methylphenyl)-3-pyrrolidinyl 221 Et CH1-(4-methylphenyl)-3-pyrrolidinyl 222 Et CH1-(2-methoxyphenyl)-3-pyrrolidinyl 223 Et CH1-(3-methoxyphenyl)-3-pyrrolidinyl 224 Et CH1-(4-methoxyphenyl)-3-pyrrolidinyl 225 Et CH1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 226 Et CH1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 227 Et CH1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 228 Et CH1-(3,5-difluorophenyl)-3-pyrrolidinyl 229 Et CH1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 230 Et CH1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 231 Et CH1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 232 Et CH1-(2-pyridyl)-3-pyrrolidinyl 233 Et CH 1-(3-pyridyl)-3-pyrrolidinyl 234Et CH 1-(4-pyridyl)-3-pyrrolidinyl 235 Et CH1-(2-pyrimidinyl)-3-pyrrolidinyl 236 Et CH 5-oxo-1-phenyl-3-pyrrolidinyl237 Et CH 1-phenyl-3-piperidyl 238 Et CH 1-(2-fluorophenyl)-3-piperidyl239 Et CH 1-(3-fluorophenyl)-3-piperidyl 240 Et CH1-(4-fluorophenyl)-3-piperidyl 241 Et CH 1-(2-chlorophenyl)-3-piperidyl242 Et CH 1-(3-chlorophenyl)-3-piperidyl 243 Et CH1-(4-chlorophenyl)-3-piperidyl 244 Et CH 1-(2-methylphenyl)-3-piperidyl245 Et CH 1-(3-methylphenyl)-3-piperidyl 246 Et CH1-(4-methylphenyl)-3-piperidyl 247 Et CH 1-(2-methoxyphenyl)-3-piperidyl248 Et CH 1-(3-methoxyphenyl)-3-piperidyl 249 Et CH1-(4-methoxyphenyl)-3-piperidyl 250 Et CH1-(2-trifluoromethylphenyl)-3-piperidyl 251 Et CH1-(3-trifluoromethylphenyl)-3-piperidyl 252 Et CH1-(4-trifluoromethylphenyl)-3-piperidyl 253 Et CH1-(3,5-difluorophenyl)-3-piperidyl 254 Et CH1-(2-difluoromethoxyphenyl)-3-piperidyl 255 Et CH1-(3-difluoromethoxyphenyl)-3-piperidyl 256 Et CH1-(4-difluoromethoxyphenyl)-3-piperidyl 257 Et CH1-(2-pyridyl)-3-piperidyl 258 Et CH 1-(3-pyridyl)-3-piperidyl 259 Et CH1-(4-pyridyl)-3-piperidyl 260 Et CH 1-phenyl-4-piperidyl 261 Et CH1-(2-fluorophenyl)-4-piperidyl 262 Et CH 1-(3-fluorophenyl)-4-piperidyl263 Et CH 1-(4-fluorophenyl)-4-piperidyl 264 Et CH1-(2-chloropheny)-4-piperidyl 265 Et CH 1-(3-chloropheny)-4-piperidyl266 Et CH 1-(4-chloropheny)-4-piperidyl 267 Et CH1-(2-methylpheny)-4-piperidyl 268 Et CH 1-(3-methylpheny)-4-piperidyl269 Et CH 1-(4-methylpheny)-4-piperidyl 270 Et CH1-(2-methoxypheny)-4-piperidyl 271 Et CH 1-(3-methoxypheny)-4-piperidyl272 Et CH 1-(4-methoxypheny)-4-piperidyl 273 Et CH1-(2-trifluoromethylpheny)-4-piperidyl 274 Et CH1-(3-trifluoromethylpheny)-4-piperidyl 275 Et CH1-(4-trifluoromethylpheny)-4-piperidyl 276 Et CH1-(3,5-difluorophenyl)-4-piperidyl 277 Et CH1-(2-difluoromethoxyphenyl)-4-piperidyl 278 Et CH1-(3-difluoromethoxyphenyl)-4-piperidyl 279 Et CH1-(4-difluoromethoxyphenyl)-4-piperidyl 280 Et CH1-(2-pyridyl)-4-piperidyl 281 Et CH 1-(3-pyridyl)-4-piperidyl 282 Et CH1-(4-pyridyl)-4-piperidyl 283 Et CH 3-hydroxymethyl-1-phenyl-4-piperidyl284 Et CH 3-methoxycarbonyl-1-phenyl-4-piperidyl 285 Et CH3-ethoxycarbonyl-1-phenyl-4-piperidyl 286 Et CH3-isopropoxycarbonyl-1-phenyl-4-piperidyl 287 Et CH 4-phenylcyclohexyl288 Et CH 4-(2-fluorophenyl)cyclohexyl 289 Et CH4-(3-fluorophenyl)cyclohexyl 290 Et CH 4-(4-fluorophenyl)cyclohexyl 291Et CH 4-(2-chlorophenyl)cyclohexyl 292 Et CH4-(3-chlorophenyl)cyclohexyl 293 Et CH 4-(4-chlorophenyl)cyclohexyl 294Et CH 4-(2-methylphenyl)cyclohexyl 295 Et CH4-(3-methylphenyl)cyclohexyl 296 Et CH 4-(4-methylphenyl)cyclohexyl 297Et CH 4-(2-methoxyphenyl)cyclohexyl 298 Et CH4-(3-methoxyphenyl)cyclohexyl 299 Et CH 4-(4-methoxyphenyl)cyclohexyl300 Et CH 4-(2-trifluoromethylphenyl)cyclohexyl 301 Et CH4-(3-trifluoromethylphenyl)cyclohexyl 302 Et CH4-(4-trifluoromethylphenyl)cyclohexyl 303 Et CH4-(3,5-difluorophenyl)cyclohexyl 304 Et CH 4-(3-acetylphenyl)cyclohexyl305 Et CH 4-(3-cyanophenyl)cyclohexyl 306 Et CH4-(2-difluoromethoxyphenyl)cyclohexyl 307 Et CH4-(3-difluoromethoxyphenyl)cyclohexyl 308 Et CH4-(4-difluoromethoxyphenyl)cyclohexyl 309 Et CH 4-(2-pyridyl)cyclohexyl310 Et CH 4-(3-pyridyl)cyclohexyl 311 Et CH 4-(4-pyridyl)cyclohexyl 312Et CH 4-(4-fluoro-3-pyridyl)cyclohexyl 313 Et CH4-(3-quinolyl)cyclohexyl 314 Et CH4-(3-fluorophenyl)-4-hydroxycyclohexyl 315 Et CH 3-phenylcyclohexyl 316Et CH 3-phenylcyclopentyl 317 Et CH 6-phenyl-3-tetrahydropyranyl 318 EtCH 6-(3-fluorophenyl)-3-tetrahydropyranyl 319 Et CH 2-phenylcyclopropyl320 Et CH 2-(2-pyridyl)cyclopropyl 321 Et CH 2-(3-pyridyl)cyclopropyl322 Et CH 2-(4-pyridyl)cyclopropyl 323 Et CH2-(3-fluorophenyl)cyclopropyl 324 Et CH 2-indanyl 325 Et CH2-tetrahydronaphthyl 326 Et CH 6-methoxy-2-tetrahydronaphthyl 327 Et CHbenzyl 328 Et CH phenethyl 329 Et CH 3-phenylpropyl 330 Et CH4-phenylbutyl 331 Et CH 2-methoxyphenethyl 332 Et CH 3-methoxyphenethyl333 Et CH 4-methoxyphenethyl 334 Et CH 4-fluorophenethyl 335 Et CH4-bromophenethyl 336 Et CH 4-chlorophenethyl 337 Et CH3-trifluoromethylphenethyl 338 Et CH 3,4-dimethoxyphenethyl 339 Et CH3-propoxyphenethyl 340 Et CH 3,5-difluorophenethyl 341 Et CH4-dimethylaminophenethyl 342 Et CH 3-difluoromethoxyphenethyl 343 Et CH2-methylphenethyl 344 Et CH 4-acetylphenethyl 345 Et CH4-dimethylamino-2-methoxyphenethyl 346 Et CH cyclohexylethyl 347 Et CH2-(2-pyridyl)ethyl 348 Et CH 2-(3-pyridyl)ethyl 349 Et CH2-(4-pyridyl)ethyl 350 Et CH 2-(2-quinolyl)ethyl 351 Et CH2-(3-quinolyl)ethyl 352 Et CH 2-(4-quinolyl)ethyl 353 Et CH2-(6-quinolyl)ethyl 354 Et CH 2-(2-indolyl)ethyl 355 Et CH2-(3-indolyl)ethyl 356 Et CH 2-(7-aza-3-indolyl)ethyl 357 Et CH2-(benzimidazolyl)ethyl 358 Et CH 2-(benzoxazolyl)ethyl 359 Et CH2-(benzothiazolyl)ethyl 360 Et CH 2-(1-naphthyl)ethyl 361 Et CH2-(2-naphthyl)ethyl 362 Et CH 1-(hydroxymethyl)-2-phenylethyl 363 Et CH1-(methoxycarbonyl)-2-phenylethyl 364 Et CH1-(ethoxycarbonyl)-2-phenylethyl 365 Et CH 1-carboxy-2-phenylethyl 366Et CH 1-(benzyloxycarbonyl)-2-phenylethyl 367 Et CH1-(phenoxymethyl)-2-phenylethyl 368 Et CH1-(benzyloxymethyl)-2-phenylethyl 369 Et CH1-(benzylcarbamoyl)-2-phenylethyl 370 Et CH1-(N-methylbenzylcarbamoyl)-2-phenylethyl 371 Et CH1-(phenylcarbamoyl)-2-phenylethyl 372 Et CH1-(N-methylphenylcarbamoyl)-2-phenylethyl 373 Et CH1-(N-benzylaminomethyl)-2-phenylethyl 374 Et CH1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 375 Et CH1-(anilinomethyl)-2-phenylethyl 376 Et CH1-(N-methylanilinomethyl)-2-phenylethyl 377 Et CH1-(N-methylaminomethyl)-2-phenylethyl 378 Et CH1-(N-ethylaxninomethyl)-2-phenylethyl 379 Et CH1-(N-isobutylaminomethyl)-2-phenylethyl 380 Et CH1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 381 Et CH1-(aminomethyl)-2-phenylethyl 382 Et CH1-benzyl-2-(2-pyridylmethylamino)ethyl 383 Et CH1-benzyl-2-(3-pyridylmethylamino)ethyl 384 Et CH1-benzyl-2-(4-pyridylmethylamino)ethyl 385 Et CH2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 386 Et CH2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 387 Et CH2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 388 Et CH2-hydroxy-2-phenylethyl 389 Et CH benzoylmethyl 390 Et CH1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 391 Et CH1-(benzyloxycarbonyl)-2-cyclohexylethyl 392 Et CH1-(phenoxymethyl)-2-(3-indolyl)ethyl 393 Et CH2-(2-methoxyphenoxyy)ethyl 394 Et CH1-(benzylcarbamoyl)-2-cyclohexylethyl 395 Et CH1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 396 Et CH1-(phenylcarbamoyl)-2-cyclohexylethyl 397 Et CH1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 398 Et CH1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 399 Et CH1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 400 Et CH1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 401 Et CH1-(4-pyridylmethylcarbamoyl)-2-(4-fluoro- phenyl)ethyl 402 Et CH1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 403 Et CH1-(benzyloxymethyl)-2-(2-indolyl)ethyl 404 Et CH1-(N-benzyl-N-methylaminomethyl)-2-(3- pyridyl)ethyl 405 Et CH1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 406 Et CH2-hydroxy-2-(4-dimethylaminophenyl)ethyl 407 Et CH2-hydroxy-2-(2-quinolyl)ethyl 408 Et CH 2-hydroxy-2-(3-quinolyl)ethyl409 Et CH 2-hydroxy-2-(4-quinolyl)ethyl 410 Et CH2-hydroxy-2-(3,5-difluorophenyl)ethyl 411 Et CH1-carboxy-2-cyclohexylethyl 412 Et CH 2-hydroxy-2-(6-quinolyl)ethyl 413Et CH 2-(benzylamino)-2-phenylethyl 414 Et CH2-amino-2-(2-naphthyl)propyl 415 Et CH 2-(phenylamino)ethyl 416 Et CHdiphenylmethyl 417 Et CH 2,2-diphenylethyl 418 Et CH2-phenyl-2-(2-pyridyl)ethyl 419 Et CH 2-phenyl-2-(3-pyridyl)ethyl 420 EtCH 2-phenyl-2-(4-pyridyl)ethyl 421 Et CH 2-phenoxy-2-phenylethyl 422 EtCH 2-(benzyloxy)-2-phenylethyl 423 Me N 1-phenyl-3-pyrrolidinyl 424 Me N1-(2-fluorophenyl)-3-pyrrolidinyl 425 Me N1-(3-fluorophenyl)-3-pyrrolidinyl 426 Me N1-(4-fluorophenyl)-3-pyrrolidinyl 427 Me N1-(2-chlorophenyl)-3-pyrrolidinyl 428 Me N1-(3-chlorophenyl)-3-pyrrolidinyl 429 Me N1-(4-chlorophenyl)-3-pyrrolidinyl 430 Me N1-(2-methylphenyl)-3-pyrrolidinyl 431 Me N1-(3-methylphenyl)-3-pyrrolidinyl 432 Me N1-(4-methylphenyl)-3-pyrrolidinyl 433 Me N1-(2-methoxyphenyl)-3-pyrrolidinyl 434 Me N1-(3-methoxyphenyl)-3-pyrrolidinyl 435 Me N1-(4-methoxyphenyl)-3-pyrrolidinyl 436 Me N1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 437 Me N1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 438 Me N1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 439 Me N1-(3,5-difluorophenyl)-3-pyrrolidinyl 440 Me N1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 441 Me N1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 442 Me N1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 443 Me N1-(2-pyridyl)-3-pyrrolidinyl 444 Me N 1-(3-pyridyl)-3-pyrrolidinyl 445Me N 1-(4-pyridyl)-3-pyrrolidinyl 446 Me N1-(2-pyrimidinyl)-3-pyrrolidinyl 447 Me N 5-oxo-1-phenyl-3-pyrrolidinyl448 Me N 1-phenyl-3-piperidyl 449 Me N 1-(2-fluorophenyl)-3-piperidyl450 Me N 1-(3-fluorophenyl)-3-piperidyl 451 Me N1-(4-fluorophenyl)-3-piperidyl 452 Me N 1-(2-chlorophenyl)-3-piperidyl453 Me N 1-(3-chlorophenyl)-3-piperidyl 454 Me N1-(4-chlorophenyl)-3-piperidyl 455 Me N 1-(2-methylphenyl)-3-piperidyl456 Me N 1-(3-methylphenyl)-3-piperidyl 457 Me N1-(4-methylphenyl)-3-piperidyl 458 Me N 1-(2-methoxyphenyl)-3-piperidyl459 Me N 1-(3-methoxyphenyl)-3-piperidyl 460 Me N1-(4-methoxyphenyl)-3-piperidyl 461 Me N1-(2-trifluoromethylphenyl)-3-piperidyl 462 Me N1-(3-trifluoromethylphenyl)-3-piperidyl 463 Me N1-(4-trifluoromethylphenyl)-3-piperidyl 464 Me N1-(3,5-difluorophenyl)-3-piperidyl 465 Me N1-(2-difluoromethoxyphenyl)-3-piperidyl 466 Me N1-(3-difluoromethoxyphenyl)-3-piperidyl 467 Me N1-(4-difluoromethoxyphenyl)-3-piperidyl 468 Me N1-(2-pyridyl)-3-piperidyl 469 Me N 1-(3-pyridyl)-3-piperidyl 470 Me N1-(4-pyridyl)-3-piperidyl 471 Me N 1-phenyl-4-piperidyl 472 Me N1-(2-fluorophenyl)-4-piperidyl 473 Me N 1-(3-fluorophenyl)-4-piperidyl474 Me N 1-(4-fluorophenyl)-4-piperidyl 475 Me N1-(2-chlorophenyl)-4-piperidyl 476 Me N 1-(3-chlorophenyl)-4-piperidyl477 Me N 1-(4-chlorophenyl)-4-piperidyl 478 Me N1-(2-methylphenyl)-4-piperidyl 479 Me N 1-(3-methylphenyl)-4-piperidyl480 Me N 1-(4-methylphenyl)-4-piperidyl 481 Me N1-(2-methoxyphenyl)-4-piperidyl 482 Me N 1-(3-methoxyphenyl)-4-piperidyl483 Me N 1-(4-methoxyphenyl)-4-piperidyl 484 Me N1-(2-trifluoromethylphenyl)-4-piperidyl 485 Me N1-(3-trifluoromethylphenyl)-4-piperidyl 486 Me N1-(4-trifluoromethylphenyl)-4-piperidyl 487 Me N1-(3,5-difluorophenyl)-4-piperidyl 488 Me N1-(2-difluoromethoxyphenyl)-4-piperidyl 489 Me N1-(3-difluoromethoxyphenyl)-4-piperidyl 490 Me N1-(4-difluoromethoxyphenyl)-4-piperidyl 491 Me N1-(2-pyridyl)-4-piperidyl 492 Me N 1-(3-pyridyl)-4-piperidyl 493 Me N1-(4-pyridyl)-4-piperidyl 494 Me N 3-hydroxymethyl-1-phenyl-4-piperidyl495 Me N 3-methoxycarbonyl-1-phenyl-4-piperidyl 496 Me N3-ethoxycarbonyl-1-phenyl-4-piperidyl 497 Me N3-isopropoxycarbonyl-1-phenyl-4-piperidyl 498 Me N 4-phenylcyclohexyl499 Me N 4-(2-fluorophenyl)cyclohexyl 500 Me N4-(3-fluorophenyl)cyclohexyl 501 Me N 4-(4-fluorophenyl)cyclohexyl 502Me N 4-(2-chlorophenyl)cyclohexyl 503 Me N 4-(3-chlorophenyl)cyclohexyl504 Me N 4-(4-chlorophenyl)cyclohexyl 505 Me N4-(2-methylphenyl)cyclohexyl 506 Me N 4-(3-methylphenyl)cyclohexyl 507Me N 4-(4-methylphenyl)cyclohexyl 508 Me N 4-(2-methoxyphenyl)cyclohexyl509 Me N 4-(3-methoxyphenyl)cyclohexyl 510 Me N4-(4-methoxyphenyl)cyclohexyl 511 Me N4-(2-trifluoromethylphenyl)cyclohexyl 512 Me N4-(3-trifluoromethylphenyl)cyclohexyl 513 Me N4-(4-trifluoromethylphenyl)cyclohexyl 514 Me N4-(3,5-difluorophenyl)cyclohexyl 515 Me N 4-(3-acetylphenyl)cyclohexyl516 Me N 4-(3-cyanophenyl)cyclohexyl 517 Me N4-(2-difluoromethoxyphenyl)cyclohexyl 518 Me N4-(3-difluoromethoxyphenyl)cyclohexyl 519 Me N4-(4-difluoromethoxyphenyl)cyclohexyl 520 Me N 4-(2-pyridyl)cyclohexyl521 Me N 4-(3-pyridyl)cyclohexyl 522 Me N 4-(4-pyridyl)cyclohexyl 523 MeN 4-(4-fluoro-3-pyridyl)cyclohexyl 524 Me N 4-(3-quinolyl)cyclohexyl 525Me N 4-(3-fluorophenyl)-4-hydroxycyclohexyl 526 Me N 3-phenylcyclohexyl527 Me N 3-phenylcyclopentyl 528 Me N 6-phenyl-3-tetrahydropyranyl 529Me N 6-(3-fluorophenyl)-3-tetrahydropyranyl 530 Me N 2-phenylcyclopropyl531 Me N 2-(2-pyridyl)cyclopropyl 532 Me N 2-(3-pyridyl)cyclopropyl 533Me N 2-(4-pyridyl)cyclopropyl 534 Me N 2-(3-fluorophenyl)cyclopropyl 535Me N 2-indanyl 536 Me N 2-tetrahydronaphthyl 537 Me N6-methoxy-2-tetrahydronaphthyl 538 Me N benzyl 539 Me N phenethyl 540 MeN 3-phenylpropyl 541 Me N 4-phenylbutyl 542 Me N 2-methoxyphenethyl 543Me N 3-methoxyphenethyl 544 Me N 4-methoxyphenethyl 545 Me N4-fluorophenethyl 546 Me N 4-bromophenethyl 547 Me N 4-chlorophenethyl548 Me N 3-trifluoromethylphenethyl 549 Me N 3,4-dimethoxyphenethyl 550Me N 3-propoxyphenethyl 551 Me N 3,5-difluorophenethyl 552 Me N4-dimethylaminophenethyl 553 Me N 3-difluoromethoxyphenethyl 554 Me N2-methylphenethyl 555 Me N 4-acetylphenethyl 556 Me N4-dimethylamino-2-methoxyphenethyl 557 Me N cyclohexylethyl 558 Me N2-(2-pyridyl)ethyl 559 Me N 2-(3-pyridyl)ethyl 560 Me N2-(4-pyridyl)ethyl 561 Me N 2-(2-quinolyl)ethyl 562 Me N2-(3-quinolyl)ethyl 563 Me N 2-(4-quinolyl)ethyl 564 Me N2-(6-quinolyl)ethyl 565 Me N 2-(2-indolyl)ethyl 566 Me N2-(3-indolyl)ethyl 567 Me N 2-(7-aza-3-indolyl)ethyl 568 Me N2-(benzimidazolyl)ethyl 569 Me N 2-(benzoxazolyl)ethyl 570 Me N2-(benzothiazolyl)ethyl 571 Me N 2-(1-naphthyl)ethyl 572 Me N2-(2-naphthyl)ethyl 573 Me N 1-(hydroxymethyl)-2-phenylethyl 574 Me N1-(methoxycarbonyl)-2-phenylethyl 575 Me N1-(ethoxycarbonyl)-2-phenylethyl 576 Me N 1-carboxy-2-phenylethyl 577 MeN 1-(benzyloxycarbonyl)-2-phenylethyl 578 Me N1-(phenoxymethyl)-2-phenylethyl 579 Me N1-(benzyloxymethyl)-2-phenylethyl 580 Me N1-(benzylcarbamoyl)-2-phenylethyl 581 Me N1-(N-methylbenzylcarbamoyl)-2-phenylethyl 582 Me N1-(phenylcarbamoyl)-2-phenylethyl 583 Me N1-(N-methylphenylcarbamoyl)-2-phenylethyl 584 Me N1-(N-benzylaminomethyl)-2-phenylethyl 585 Me N1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 586 Me N1-(anilinomethyl)-2-phenylethyl 587 Me N1-(N-methylanilinomethyl)-2-phenylethyl 588 Me N1-(N-methylaminomethyl)-2-phenylethyl 589 Me N1-(N-ethylaminomethyl)-2-phenylethyl 590 Me N1-(N-isobutylaminomethyl)-2-phenylethyl 591 Me N1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 592 Me N1-(aminomethyl)-2-phenylethyl 593 Me N1-benzyl-2-(2-pyridylmethylamino)ethyl 594 Me N1-benzyl-2-(3-pyridylmethylamino)ethyl 595 Me N1-benzyl-2-(4-pyridylmethylamino)ethyl 596 Me N2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 597 Me N2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 598 Me N2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 599 Me N2-hydroxy-2-phenylethyl 600 Me N benzoylmethyl 601 Me N1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 602 Me N1-(benzyloxycarbonyl)-2-cyclohexylethyl 603 Me N1-(phenoxymethyl)-2-(3-indolyl)ethyl 604 Me N 2-(2-methoxyphenoxy)ethyl605 Me N 1-(benzylcarbamoyl)-2-cyclohexylethyl 606 Me N1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 607 Me N1-(phenylcarbamoyl)-2-cyclohexylethyl 608 Me N1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 609 Me N1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 610 Me N1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 611 Me N1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 612 Me N1-(4-pyridylmethylcarbamoyl)-2-(4-fluoro- phenyl) ethyl 613 Me N1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 614 Me N1-(benzyloxymethyl)-2-(2-indolyl)ethyl 615 Me N1-(N-benzyl-N-methylaminomethyl)-2-(3- pyridyl)ethyl 616 Me N1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 617 Me N2-hydroxy-2-(4-dimethylaminophenyl)ethyl 618 Me N2-hydroxy-2-(2-quinolyl)ethyl 619 Me N 2-hydroxy-2-(3-quinolyl)ethyl 620Me N 2-hydroxy-2-(4-quinolyl)ethyl 621 Me N2-hydroxy-2-(3,5-difluorophenyl)ethyl 622 Me N1-carboxy-2-cyclohexylethyl 623 Me N 2-hydroxy-2-(6-quinolyl)ethyl 624Me N 2-(benzylamino)-2-phenylethyl 625 Me N 2-amino-2-(2-naphthyl)propyl626 Me N 2-(phenylamino)ethyl 627 Me N diphenylmethyl 628 Me N2,2-diphenylethyl 629 Me N 2-phenyl-2-(2-pyridyl)ethyl 630 Me N2-phenyl-2-(3-pyridyl)ethyl 631 Me N 2-phenyl-2-(4-pyridyl)ethyl 632 MeN 2-phenoxy-2-phenylethyl 633 Me N 2-(benzyloxy)-2-phenylethyl 634 Et N1-phenyl-3-pyrrolidinyl 635 Et N 1-(2-fluorophenyl)-3-pyrrolidinyl 636Et N 1-(3-fluorophenyl)-3-pyrrolidinyl 637 Et N1-(4-fluorophenyl)-3-pyrrolidinyl 638 Et N1-(2-chlorophenyl)-3-pyrrolidinyl 639 Et N1-(3-chlorophenyl)-3-pyrrolidinyl 640 Et N1-(4-chlorophenyl)-3-pyrrolidinyl 641 Et N1-(2-methylphenyl)-3-pyrrolidinyl 642 Et N1-(3-methylphenyl)-3-pyrrolidinyl 643 Et N1-(4-methylphenyl)-3-pyrrolidinyl 644 Et N1-(2-methoxyphenyl)-3-pyrrolidinyl 645 Et N1-(3-methoxyphenyl)-3-pyrrolidinyl 646 Et N1-(4-methoxyphenyl)-3-pyrrolidinyl 647 Et N1-(2-trifluoromethylphenyl)-3-pyrrolidinyl 648 Et N1-(3-trifluoromethylphenyl)-3-pyrrolidinyl 649 Et N1-(4-trifluoromethylphenyl)-3-pyrrolidinyl 650 Et N1-(3,5-difluorophenyl)-3-pyrrolidinyl 651 Et N1-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 652 Et N1-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 653 Et N1-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 654 Et N1-(2-pyridyl)-3-pyrrolidinyl 655 Et N 1-(3-pyridyl)-3-pyrrolidinyl 656Et N 1-(4-pyridyl)-3-pyrrolidinyl 657 Et N1-(2-pyrimidinyl)-3-pyrrolidinyl 658 Et N 5-oxo-1-phenyl-3-pyrrolidinyl659 Et N 1-phenyl-3-piperidyl 660 Et N 1-(2-fluorophenyl)-3-piperidyl661 Et N 1-(3-fluorophenyl)-3-piperidyl 662 Et N1-(4-fluorophenyl)-3-piperidyl 663 Et N 1-(2-chlorophenyl)-3-piperidyl664 Et N 1-(3-chlorophenyl)-3-piperidyl 665 Et N1-(4-chlorophenyl)-3-piperidyl 666 Et N 1-(2-methylphenyl)-3-piperidyl667 Et N 1-(3-methylphenyl)-3-piperidyl 668 Et N1-(4-methylphenyl)-3-piperidyl 669 Et N 1-(2-methoxyphenyl)-3-piperidyl670 Et N 1-(3-methoxyphenyl)-3-piperidyl 671 Et N1-(4-methoxyphenyl)-3-piperidyl 672 Et N1-(2-trifluoromethylphenyl)-3-piperidyl 673 Et N1-(3-trifluoromethylphenyl)-3-piperidyl 674 Et N1-(4-trifluoromethylphenyl)-3-piperidyl 675 Et N1-(3,5-difluorophenyl)-3-piperidyl 676 Et N1-(2-difluoromethoxyphenyl)-3-piperidyl 677 Et N1-(3-difluoromethoxyphenyl)-3-piperidyl 678 Et N1-(4-difluoromethoxyphenyl)-3-piperidyl 679 Et N1-(2-pyridyl)-3-piperidyl 680 Et N 1-(3-pyridyl)-3-piperidyl 681 Et N1-(4-pyridyl)-3-piperidyl 682 Et N 1-phenyl-4-piperidyl 683 Et N1-(2-fluorophenyl)-4-piperidyl 684 Et N 1-(3-fluorophenyl)-4-piperidyl685 Et N 1-(4-fluorophenyl)-4-piperidyl 686 Et N1-(2-chlorophenyl)-4-piperidyl 687 Et N 1-(3-chlorophenyl)-4-piperidyl688 Et N 1-(4-chlorophenyl)-4-piperidyl 689 Et N1-(2-methylphenyl)-4-piperidyl 690 Et N 1-(3-methylphenyl)-4-piperidyl691 Et N 1-(4-methylphenyl)-4-piperidyl 692 Et N1-(2-methoxyphenyl)-4-piperidyl 693 Et N 1-(3-methoxyphenyl)-4-piperidyl694 Et N 1-(4-methoxyphenyl)-4-piperidyl 695 Et N1-(2-trifluoromethylphenyl)-4-piperidyl 696 Et N1-(3-trifluoromethylphenyl)-4-piperidyl 697 Et N1-(4-trifluoromethylphenyl)-4-piperidyl 698 Et N1-(3,5-difluorophenyl)-4-piperidyl 699 Et N1-(2-difluoromethoxyphenyl)-4-piperidyl 700 Et N1-(3-difluoromethoxyphenyl)-4-piperidyl 701 Et N1-(4-difluoromethoxyphenyl)-4-piperidyl 702 Et N1-(2-pyridyl)-4-piperidyl 703 Et N 1-(3-pyridyl)-4-piperidyl 704 Et N1-(4-pyridyl)-4-piperidyl 705 Et N 3-hydroxymethyl-1-phenyl-4-piperidyl706 Et N 3-methoxycarbonyl-1-phenyl-4-piperidyl 707 Et N3-ethoxycarbonyl-1-phenyl-4-piperidyl 708 Et N3-isopropoxycarbonyl-1-phenyl-4-piperidyl 709 Et N 4-phenylcyclohexyl710 Et N 4-(2-fluorophenyl)cyclohexyl 711 Et N4-(3-fluorophenyl)cyclohexyl 712 Et N 4-(4-fluorophenyl)cyclohexyl 713Et N 4-(2-chlorophenyl)cyclohexyl 714 Et N 4-(3-chlorophenyl)cyclohexyl715 Et N 4-(4-chlorophenyl)cyclohexyl 716 Et N4-(2-methylphenyl)cyclohexyl 717 Et N 4-(3-methylphenyl)cyclohexyl 718Et N 4-(4-methylphenyl)cyclohexyl 719 Et N 4-(2-methoxyphenyl)cyclohexyl720 Et N 4-(3-methoxyphenyl)cyclohexyl 721 Et N4-(4-methoxyphenyl)cyclohexyl 722 Et N4-(2-trifluoromethylphenyl)cyclohexyl 723 Et N4-(3-trifluoromethylphenyl)cyclohexyl 724 Et N4-(4-trifluoromethylphenyl)cyclohexyl 725 Et N4-(3,5-difluorophenyl)cyclohexyl 726 Et N 4-(3-acetylphenyl)cyclohexyl727 Et N 4-(3-cyanophenyl)cyclohexyl 728 Et N4-(2-difluoromethoxyphenyl)cyclohexyl 729 Et N4-(3-difluoromethoxyphenyl)cyclohexyl 730 Et N4-(4-difluoromethoxyphenyl)cyclohexyl 731 Et N 4-(2-pyridyl)cyclohexyl732 Et N 4-(3-pyridyl)cyclohexyl 733 Et N 4-(4-pyridyl)cyclohexyl 734 EtN 4-(4-fluoro-3-pyridyl)cyclohexyl 735 Et N 4-(3-quinolyl)cyclohexyl 736Et N 4-(3-fluorophenyl)-4-hydroxycyclohexyl 737 Et N 3-phenylcyclohexyl738 Et N 3-phenylcyclopentyl 739 Et N 6-phenyl-3-tetrahydropyranyl 740Et N 6-(3-fluorophenyl)-3-tetrahydropyranyl 741 Et N 2-phenylcyclopropyl742 Et N 2-(2-pyridyl)cyclopropyl 743 Et N 2-(3-pyridyl)cyclopropyl 744Et N 2-(4-pyridyl)cyclopropyl 745 Et N 2-(3-fluorophenyl)cyclopropyl 746Et N 2-indanyl 747 Et N 2-tetrahydronaphthyl 748 Et N6-methoxy-2-tetrahydronaphthyl 749 Et N benzyl 750 Et N phenethyl 751 EtN 3-phenylpropyl 752 Et N 4-phenylbutyl 753 Et N 2-methoxyphenethyl 754Et N 3-methoxyphenethyl 755 Et N 4-methoxyphenethyl 756 Et N4-fluorophenethyl 757 Et N 4-bromophenethyl 758 Et N 4-chlorophenethyl759 Et N 3-trifluoromethylphenethyl 760 Et N 3,4-dimethoxyphenethyl 761Et N 3-propoxyphenethyl 762 Et N 3,5-difluorophenethyl 763 Et N4-dimethylaminophenethyl 764 Et N 3-difluoromethoxyphenethyl 765 Et N2-methylphenethyl 766 Et N 4-acetylphenethyl 767 Et N4-dimethylamino-2-methoxyphenethyl 768 Et N cyclohexylethyl 769 Et N2-(2-pyridyl)ethyl 770 Et N 2-(3-pyridyl)ethyl 771 Et N2-(4-pyridyl)ethyl 772 Et N 2-(2-quinolyl)ethyl 773 Et N2-(3-quinolyl)ethyl 774 Et N 2-(4-quinolyl)ethyl 775 Et N2-(6-quinolyl)ethyl 776 Et N 2-(2-indolyl)ethyl 777 Et N2-(3-indolyl)ethyl 778 Et N 2-(7-aza-3-indolyl)ethyl 779 Et N2-(benzimidazolyl)ethyl 780 Et N 2-(benzoxazolyl)ethyl 781 Et N2-(benzothiazolyl)ethyl 782 Et N 2-(1-naphthyl)ethyl 783 Et N2-(2-naphthyl)ethyl 784 Et N 1-(hydroxymethyl)-2-phenylethyl 785 Et N1-(methoxycarbonyl)-2-phenylethyl 786 Et N1-(ethoxycarbonyl)-2-phenylethyl 787 Et N 1-carboxy-2-phenylethyl 788 EtN 1-(benzyloxycarbonyl)-2-phenylethyl 789 Et N1-(phenoxymethyl)-2-phenylethyl 790 Et N1-(benzyloxymethyl)-2-phenylethyl 791 Et N1-(benzylcarbamoyl)-2-phenylethyl 792 Et N1-(N-methylbenzylcarbamoyl)-2-phenylethyl 793 Et N1-(phenylcarbamoyl)-2-phenylethyl 794 Et N1-(N-methylphenylcarbamoyl)-2-phenylethyl 795 Et N1-(N-benzylaminomethyl)-2-phenylethyl 796 Et N1-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 797 Et N1-(anilinomethyl)-2-phenylethyl 798 Et N1-(N-methylanilinomethyl)-2-phenylethyl 799 Et N1-(N-methylaminomethyl)-2-phenylethyl 800 Et N1-(N-ethylaminomethyl)-2-phenylethyl 801 Et N1-(N-isobutylaminomethyl)-2-phenylethyl 802 Et N1-(N-cyclopropylmethylaminomethyl)-2-phenyl- ethyl 803 Et N1-(aminomethyl)-2-phenylethyl 804 Et N1-benzyl-2-(2-pyridylmethylamino)ethyl 805 Et N1-benzyl-2-(3-pyridylmethylamino)ethyl 806 Et N1-benzyl-2-(4-pyridylmethylamino)ethyl 807 Et N2-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 808 Et N2-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 809 Et N2-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 810 Et N2-hydroxy-2-phenylethyl 811 Et N benzoylmethyl 812 Et N1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 813 Et N1-(benzyloxycarbonyl)-2-cyclohexylethyl 814 Et N1-(phenoxymethyl)-2-(3-indolyl)ethyl 815 Et N 2-(2-methoxyphenoxy)ethyl816 Et N 1-(benzylcarbamoyl)-2-cyclohexylethyl 817 Et N1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 818 Et N1-(phenylcarbamoyl)-2-cyclohexylethyl 819 Et N1-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 820 Et N1-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 821 Et N1-(benzylaminomethyl)-2-(3-pyridyl)ethyl 822 Et N1-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 823 Et N1-(4-pyridylmethylcarbamoyl)-2-(4-fluoro- phenyl)ethyl 824 Et N1-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 825 Et N1-(benzyloxymethyl)-2-(2-indolyl)ethyl 826 Et N1-(N-benzyl-N-methylaminomethyl)-2-(3- pyridyl)ethyl 827 Et N1-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 828 Et N2-hydroxy-2-(4-dimethylaminophenyl)ethyl 829 Et N2-hydroxy-2-(2-quinolyl)ethyl 830 Et N 2-hydroxy-2-(3-quinolyl)ethyl 831Et N 2-hydroxy-2-(4-quinolyl)ethyl 832 Et N2-hydroxy-2-(3,5-difluorophenyl)ethyl 833 Et N1-carboxy-2-cyclohexylethyl 834 Et N 2-hydroxy-2-(6-quinolyl)ethyl 835Et N 2-(benzylamino)-2-phenylethyl 836 Et N 2-amino-2-(2-naphthyl)propyl837 Et N 2-(phenylamino)ethyl 838 Et N diphenylmethyl 839 Et N2,2-diphenylethyl 840 Et N 2-phenyl-2-(2-pyridyl)ethyl 841 Et N2-phenyl-2-(3-pyridyl)ethyl 842 Et N 2-phenyl-2-(4-pyridyl)ethyl 843 EtN 2-phenoxy-2-phenylethyl 844 Et N 2-(benzyloxy)-2-phenylethyl

TABLE 2

No. A—Ar¹—R⁰ 845 1-phenyl-3-pyrrolidinyl 8461-(2-fluorophenyl)-3-pyrrolidinyl 847 1-(3-fluorophenyl)-3-pyrrolidinyl848 1-(4-fluorophenyl)-3-pyrrolidinyl 8491-(2-chlorophenyl)-3-pyrrolidinyl 850 1-(3-chlorophenyl)-3-pyrrolidinyl851 1-(4-chlorophenyl)-3-pyrrolidinyl 8521-(2-methylphenyl)-3-pyrrolidinyl 853 1-(3-methylphenyl)-3-pyrrolidinyl854 1-(4-methylphenyl)-3-pyrrolidinyl 8551-(2-methoxphenyl)-3-pyrrolidinyl 856 1-(3-methylphenyl)-3-pyrrolidinyl857 1-(4-methylphenyl)-3-pyrrolidinyl 8581-(2-trifluoromethylphenyl)-3-pyrrolidinyl 8591-(3-trifluoromethylphenyl)-3-pyrrolidinyl 8601-(4-trifluoromethylphenyl)-3-pyrrolidinyl 8611-(3,5-difluorophenyl)-3-pyrrolidinyl 8621-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 8631-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 8641-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 8651-(2-pyridyl)-3-pyrrolidinyl 866 1-(3-pyridyl)-3-pyrrolidinyl 8671-(4-pyridyl)-3-pyrrolidinyl 868 1-(2-pyrimidinyl)-3-pyrrolidinyl 8695-oxo-1-phenyl-3-pyrrolidinyl 870 1-phenyl-3-piperidyl 8711-(2-fluorophenyl)-3-piperidyl 872 1-(3-fluorophenyl)-3-piperidyl 8731-(4-fluorophenyl)-3-piperidyl 874 1-(2-chlorophenyl)-3-piperidyl 8751-(3-chlorophenyl)-3-piperidyl 876 1-(4-chlorophenyl)-3-piperidyl 8771-(2-methylphenyl)-3-piperidyl 878 1-(3-methylphenyl)-3-piperidyl 8791-(4-methylphenyl)-3-piperidyl 880 1-(2-methoxyphenyl)-3-piperidyl 8811-(3-methoxyphenyl)-3-piperidyl 882 1-(4-methoxyphenyl)-3-piperidyl 8831-(2-trifluoromethylphenyl)-3-piperidyl 8841-(3-trifluoromethylphenyl)-3-piperidyl 8851-(4-trifluoromethylphenyl)-3-piperidyl 8861-(3,5-difluorophenyl)-3-piperidyl 8871-(2-difluoromethoxyphenyl)-3-piperidyl 8881-(3-difluoromethoxyphenyl)-3-piperidyl 8891-(4-difluoromethoxyphenyl)-3-piperidyl 890 1-(2-pyridyl)-3-piperidyl891 1-(3-pyridyl)-3-piperidyl 892 1-(4-pyridyl)-3-piperidyl 8931-phenyl-4-piperidyl 894 1-(2-fluorophenyl)-4-piperidyl 8951-(3-fluorophenyl)-4-piperidyl 896 1-(4-fluorophenyl)-4-piperidyl 8971-(2-chlorophenyl)-4-piperidyl 898 1-(3-chlorophenyl)-4-piperidyl 8991-(4-chlorophenyl)-4-piperidyl 900 1-(2-methylphenyl)-4-piperidyl 9011-(3-methylphenyl)-4-piperidyl 902 1-(4-methylphenyl)-4-piperidyl 9031-(2-methoxyphenyl)-4-piperidyl 904 1-(3-methoxyphenyl)-4-piperidyl 9051-(4-methoxyphenyl)-4-piperidyl 9061-(2-trifluoromethylphenyl)-4-piperidyl 9071-(3-trifluoromethylphenyl)-4-piperidyl 9081-(4-trifluoromethylphenyl)-4-piperidyl 9091-(3,5-difluorophenyl)-4-piperidyl 9101-(2-difluoromethoxyphenyl)-4-piperidyl 9111-(3-difluoromethoxyphenyl)-4-piperidyl 9121-(4-difluoromethoxyphenyl)-4-piperidyl 913 1-(2-pyridyl)-4-piperidyl914 1-(3-pyridyl)-4-piperidyl 915 1-(4-pyridyl)-4-piperidyl 9163-hydroxymethyl-1-phenyl-4-piperidyl 9173-methoxycarbonyl-1-phenyl-4-piperidyl 9183-ethoxycarbonyl-1-phenyl-4-piperidyl 9193-isopropoxycarbonyl-1-phenyl-4-piperidyl 920 4-phenylcyclohexyl 9214-(2-fluorophenyl)cyclohexyl 922 4-(3-fluorophenyl)cyclohexyl 9234-(4-fluorophenyl)cyclohexyl 924 4-(2-chlorophenyl)cyclohexyl 9254-(3-chlorophenyl)cyclohexyl 926 4-(4-chlorophenyl)cyclohexyl 9274-(2-methylphenyl)cyclohexyl 928 4-(3-methylphenyl)cyclohexyl 9294-(4-methylphenyl)cyclohexyl 930 4-(2-methoxyphenyl)cyclohexyl 9314-(3-methoxyphenyl)cyclohexyl 932 4-(4-methoxyphenyl)cyclohexyl 9334-(2-trifluoromethylphenyl)cyclohexyl 9344-(3-trifluoromethylphenyl)cyclohexyl 9354-(4-trifluoromethylphenyl)cyclohexyl 9364-(3,5-difluorophenyl)cyclohexyl 937 4-(3-acetylphenyl)cyclohexyl 9384-(3-cyanophenyl)cyclohexyl 939 4-(2-difluoromethoxyphenyl)cyclohexyl940 4-(3-difluoromethoxyphenyl)cyclohexyl 9414-(4-difluoromethoxyphenyl)cyclohexyl 942 4-(2-pyridyl)cyclohexyl 9434-(3-pyridyl)cyclohexyl 944 4-(4-pyridyl)cyclohexyl 9454-(4-fluoro-3-pyridyl)cyclohexyl 946 4-(3-quinolyl)cyclohexyl 9474-(3-fluorophenyl)-4-hydroxycyclohexyl 948 3-phenylcyclohexyl 9493-phenylcyclopentyl 950 6-phenyl-3-tetrahydropyranyl 9516-(3-fluorophenyl)-3-tetrahydropyranyl 952 2-phenylcyclopropyl 9532-(2-pyridyl)cyclopropyl 954 2-(3-pyridyl)cyclopropyl 9552-(4-pyridyl)cyclopropyl 956 2-(3-fluorophenyl)cyclopropyl 957 2-indanyl958 2-tetrahydronaphthyl 959 6-methoxy-2-tetrahydronaphthyl 960 benzyl961 phenethyl 962 3-phenylpropyl 963 4-phenylbutyl 9642-methoxyphenethyl 965 3-methoxyphenethyl 966 4-methoxyphenethyl 9674-fluorophenethyl 968 4-bromophenethyl 969 4-chlorophenethyl 9703-trifluoromethylphenethyl 971 3,4-dimethoxyphenethyl 9723-propoxyphenethyl 973 3,5-difluorophenethyl 9744-dimethylaminophenethyl 975 3-difluoromethoxyphenethyl 9762-methylphenethyl 977 4-acetylphenethyl 9784-dimethylamino-2-methoxyphenethyl 979 cyclohexylethyl 9802-(2-pyridyl)ethyl 981 2-(3-pyridyl)ethyl 982 2-(4-pyridyl)ethyl 9832-(2-quinolyl)ethyl 984 2-(3-quinolyl)ethyl 985 2-(4-quinolyl)ethyl 9862-(6-quinolyl)ethyl 987 2-(2-indolyl)ethyl 988 2-(3-indolyl)ethyl 9892-(7-aza-3-indolyl)ethyl 990 2-(benzimidazolyl)ethyl 9912-(benzoxazolyl)ethyl 992 2-(benzothiazolyl)ethyl 9932-(1-naphthyl)ethyl 994 2-(2-naphthyl)ethyl 9951-(hydroxymethyl)-2-phenylethyl 996 1-(methoxycarbonyl)-2-phenylethyl997 1-(ethoxycarbonyl)-2-phenylethyl 998 1-carboxy-2-phenylethyl 9991-(benzyloxycarbonyl)-2-phenylethyl 1000 1-(phenoxymethyl)-2-phenylethyl1001 1-(benzyloxymethyl)-2-phenylethyl 10021-(benzylcarbamoyl)-2-phenylethyl 10031-(N-methylbenzylcarbamoyl)-2-phenylethyl 10041-(phenylcarbamoyl)-2-phenylethyl 10051-(N-methylphenylcarbamoyl)-2-phenylethyl 10061-(N-benzylaminomethyl)-2-phenylethyl 10071-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 10081-(anilinomethyl)-2-phenylethyl 10091-(N-methylanilinomethyl)-2-phenylethyl 10101-(N-methylaminomethyl)-2-phenylethyl 10111-(N-ethylaminomethyl)-2-phenylethyl 10121-(N-isobutylaminomethyl)-2-phenylethyl 10131-(N-cyclopropylmethylaminomethyl)-2-phenylethyl 10141-(aminomethyl)-2-phenylethyl 10151-benzyl-2-(2-pyridylmethylamino)ethyl 10161-benzyl-2-(3-pyridylmethylamino)ethyl 10171-benzyl-2-(4-pyridylmethylamino)ethyl 10182-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 10192-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 10202-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 1021 2-hydroxy-2-phenylethyl1022 benzoylmethyl 1023 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 10241-(benzyloxycarbonyl)-2-cyclohexylethyl 10251-(phenoxymethyl)-2-(3-indolyl)ethyl 1026 2-(2-methoxyphenoxy)ethyl 10271-(benzylcarbamoyl)-2-cyclohexylethyl 10281-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 10291-(phenylcarbamoyl)-2-cyclohexylethyl 10301-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 10311-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 10321-(benzylaminomethyl)-2-(3-pyridyl)ethyl 10331-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 10341-(4-pyridylmethylcarbamoyl)-2-(4-fluorophenyl)ethyl 10351-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 10361-(benzyloxymethyl)-2-(2-indolyl)ethyl 10371-(N-benzyl-N-methylaminomethyl)-2-(3-pyridyl)ethyl 10381-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 10392-hydroxy-2-(4-dimethylaminophenyl)ethyl 10402-hydroxy-2-(2-quinolyl)ethyl 1041 2-hydroxy-2-(3-quinolyl)ethyl 10422-hydroxy-2-(4-quinolyl)ethyl 1043 2-hydroxy-2-(3,5-difluorophenyl)ethyl1044 1-carboxy-2-cyclohexylethyl 1045 2-hydroxy-2-(6-quinolyl)ethyl 10462-(benzylamino)-2-phenylethyl 1047 2-amino-2-(2-naphthyl)propyl 10482-(phenylamino)ethyl 1049 diphenylmethyl 1050 2,2-diphenylethyl 10512-phenyl-2-(2-pyridyl)ethyl 1052 2-phenyl-2-(3-pyridyl)ethyl 10532-phenyl-2-(4-pyridyl)ethyl 1054 2-phenoxy-2-phenylethyl 10552-(benzyloxy)-2-phenylethyl

TABLE 3

No. T U V W Z A—Ar¹—R⁰ 1056 CH CH CH CH CH 1-phenyl-3-pyrrolidinyl 1057CH CH CH CH CH 1-(2-fluorophenyl)-3- pyrrolidinyl 1058 CH CH CH CH CH1-(3-fluorophenyl)-3- pyrrolidinyl 1059 CH CH CH CH CH1-(4-fluorophenyl)-3- pyrrolidinyl 1060 CH CH CH CH CH1-(2-chlorophenyl)-3- pyrrolidinyl 1061 CH CH CH CH CH1-(3-chlorophenyl)-3- pyrrolidinyl 1062 CH CH CH CH CH1-(4-chlorophenyl)-3- pyrrolidinyl 1063 CH CH CH CH CH1-(2-methylphenyl)-3- pyrrolidinyl 1064 CH CH CH CH CH1-(3-methylphenyl)-3- pyrrolidinyl 1065 CH CH CH CH CH1-(4-methylphenyl)-3- pyrrolidinyl 1066 CH CH CH CH CH1-(2-methoxyyphenyl)-3- pyrrolidinyl 1067 CH CH CH CH CH1-(3-methoxyyphenyl)-3- pyrrolidinyl 1068 CH CH CH CH CH1-(4-methoxyyphenyl)-3- pyrrolidinyl 1069 CH CH CH CH CH1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1070 CH CH CH CH CH1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1071 CH CH CH CH CH1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1072 CH CH CH CH CH1-(3,5-difluorophenyl)-3- pyrrolidinyl 1073 CH CH CH CH CH1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1074 CH CH CH CH CH1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1075 CH CH CH CH CH1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1076 CH CH CH CH CH1-(2-pyridyl)-3-pyrrolidinyl 1077 CH CH CH CH CH1-(3-pyridyl)-3-pyrrolidinyl 1078 CH CH CH CH CH1-(4-pyridyl)-3-pyrrolidinyl 1079 CH CH CH CH CH1-(2-pyrimidinyl)-3-pyrrolidinyl 1080 CH CH CH CH CH5-oxo-1-phenyl-3-pyrrolidinyl 1081 CH CH CH CH CH 1-phenyl-3-piperidyl1082 CH CH CH CH CH 1-(2-fluorophenyl)-3-piperidyl 1083 CH CH CH CH CH1-(3-fluorophenyl)-3-piperidyl 1084 CH CH CH CH CH1-(4-fluorophenyl)-3-piperidyl 1085 CH CH CH CH CH1-(2-chlorophenyl)-3-piperidyl 1086 CH CH CH CH CH1-(3-chlorophenyl)-3-piperidyl 1087 CH CH CH CH CH1-(4-chlorophenyl)-3-piperidyl 1088 CH CH CH CH CH1-(2-methylphenyl)-3-piperidyl 1089 CH CH CH CH CH1-(3-methylphenyl)-3-piperidyl 1090 CH CH CH CH CH1-(4-methylphenyl)-3-piperidyl 1091 CH CH CH CH CH1-(2-methoxyphenyl)-3-piperidyl 1092 CH CH CH CH CH1-(3-methoxyphenyl)-3-piperidyl 1093 CH CH CH CH CH1-(4-methoxyphenyl)-3-piperidyl 1094 CH CH CH CH CH1-(2-trifluoromethylphenyl)-3- piperidyl 1095 CH CH CH CH CH1-(3-trifluoromethylphenyl)-3- piperidyl 1096 CH CH CH CH CH1-(4-trifluoromethylphenyl)-3- piperidyl 1097 CH CH CH CH CH1-(3,5-difluorophenyl)-3-piperidyl 1098 CH CH CH CH CH1-(2-difluoromethoxyphenyl)-3- piperidyl 1099 CH CH CH CH CH1-(3-difluoromethoxyphenyl)-3- piperidyl 1100 CH CH CH CH CH1-(4-difluoromethoxyphenyl)-3- piperidyl 1101 CH CH CH CH CH1-(2-pyridyl)-3-piperidyl 1102 CH CH CH CH CH 1-(3-pyridyl)-3-piperidyl1103 CH CH CH CH CH 1-(4-pyridyl)-3-piperidyl 1104 CH CH CH CH CH1-phenyl-4-piperidyl 1105 CH CH CH CH CH 1-(2-fluorophenyl)-4-piperidyl1106 CH CH CH CH CH 1-(3-fluorophenyl)-4-piperidyl 1107 CH CH CH CH CH1-(4-fluorophenyl)-4-piperidyl 1108 CH CH CH CH CH1-(2-chlorophenyl)-4-piperidyl 1109 CH CH CH CH CH1-(3-chlorophenyl)-4-piperidyl 1110 CH CH CH CH CH1-(4-chlorophenyl)-4-piperidyl 1111 CH CH CH CH CH1-(2-methylphenyl)-4-piperidyl 1112 CH CH CH CH CH1-(3-methylphenyl)-4-piperidyl 1113 CH CH CH CH CH1-(4-methylphenyl)-4-piperidyl 1114 CH CH CH CH CH1-(2-methoxyphenyl)-4-piperidyl 1115 CH CH CH CH CH1-(3-methoxyphenyl)-4-piperidyl 1116 CH CH CH CH CH1-(4-methoxyphenyl)-4-piperidyl 1117 CH CH CH CH CH1-(2-trifluoromethylphenyl)-4- piperidyl 1118 CH CH CH CH CH1-(3-trifluoromethylphenyl)-4- piperidyl 1119 CH CH CH CH CH1-(4-trifluoromethylphenyl)-4- piperidyl 1120 CH CH CH CH CH1-(3,5-difluorophenyl)-4-piperidyl 1121 CH CH CH CH CH1-(2-difluoromethoxyphenyl)-4- piperidyl 1122 CH CH CH CH CH1-(3-difluoromethoxyphenyl)-4- piperidyl 1123 CH CH CH CH CH1-(4-difluoromethoxyphenyl)-4- piperidyl 1124 CH CH CH CH CH1-(2-pyridyl)-4-piperidyl 1125 CH CH CH CH CH 1-(3-pyridyl)-4-piperidyl1126 CH CH CH CH CH 1-(4-pyridyl)-4-piperidyl 1127 CH CH CH CH CH3-hydroxymethyl-1-phenyl-4- piperidyl 1128 CH CH CH CH CH3-methoxycarbonyl-1-phenyl-4- piperidyl 1129 CH CH CH CH CH3-ethoxycarbonyl-1-phenyl-4- piperidyl 1130 CH CH CH CH CH3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1131 CH CH CH CH CH4-phenylcyclohexyl 1132 CH CH CH CH CH 4-(2-fluorophenyl)cyclohexyl 1133CH CH CH CH CH 4-(3-fluorophenyl)cyclohexyl 1134 CH CH CH CH CH4-(4-fluorophenyl)cyclohexyl 1135 CH CH CH CH CH4-(2-chlorophenyl)cyclohexyl 1136 CH CH CH CH CH4-(3-chlorophenyl)cyclohexyl 1137 CH CH CH CH CH4-(4-chlorophenyl)cyclohexyl 1138 CH CH CH CH CH4-(2-methylphenyl)cyclohexyl 1139 CH CH CH CH CH4-(3-methylphenyl)cyclohexyl 1140 CH CH CH CH CH4-(4-methylphenyl)cyclohexyl 1141 CH CH CH CH CH4-(2-methoxyphenyl)cyclohexyl 1142 CH CH CH CH CH4-(3-methoxyphenyl)cyclohexyl 1143 CH CH CH CH CH4-(4-methoxyphenyl)cyclohexyl 1144 CH CH CH CH CH4-(2-trifluoromethylphenyl)cyclo- hexyl 1145 CH CH CH CH CH4-(3-trifluoromethylphenyl)cyclo- hexyl 1146 CH CH CH CH CH4-(4-trifluoromethylphenyl)cyclo- hexyl 1147 CH CH CH CH CH4-(3,5-difluorophenyl)cyclohexyl 1148 CH CH CH CH CH4-(3-acetylphenyl)cyclohexyl 1149 CH CH CH CH CH4-(3-cyanophenyl)cyclohexyl 1150 CH CH CH CH CH4-(2-difluoromethoxyphenyl)cyclo- hexyl 1151 CH CH CH CH CH4-(3-difluoromethoxyphenyl)cyclo- hexyl 1152 CH CH CH CH CH4-(4-difluoromethoxyphenyl)cyclo- hexyl 1153 CH CH CH CH CH4-(2-pyridyl)cyclohexyl 1154 CH CH CH CH CH 4-(3-pyridyl)cyclohexyl 1155CH CH CH CH CH 4-(4-pyridyl)cyclohexyl 1156 CH CH CH CH CH4-(4-fluoro-3-pyridyl)cyclohexyl 1157 CH CH CH CH CH4-(3-quinolyl)cyclohexyl 1158 CH CH CH CH CH4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 1159 CH CH CH CH CH3-phenylcyclohexyl 1160 CH CH CH CH CH 3-phenylcyclopentyl 1161 CH CH CHCH CH 6-phenyl-3-tetrhydropyranyl 1162 CH CH CH CH CH6-(3-fluorophenyl)-3-tetrhydro- pyranyl 1163 CH CH CH CH CH2-phenylcyclopropyl 1164 CH CH CH CH CH 2-(2-pyridyl)cyclopropyl 1165 CHCH CH CH CH 2-(3-pyridyl)cyclopropyl 1166 CH CH CH CH CH2-(4-pyridyl)cyclopropyl 1167 CH CH CH CH CH2-(3-fluorophenyl)cyclopropyl 1168 CH CH CH CH CH 2-indanyl 1169 CH CHCH CH CH 2-tetrahydronaphthyl 1170 CH CH CH CH CH6-methoxy-2-tetrahydronaphthyl 1171 CH CH CH CH CH benzyl 1172 CH CH CHCH CH phenethyl 1173 CH CH CH CH CH 3-phenylpropyl 1174 CH CH CH CH CH4-phenylbutyl 1175 CH CH CH CH CH 2-methoxyphenethyl 1176 CH CH CH CH CH3-methoxyphenethyl 1177 CH CH CH CH CH 4-methoxyphenethyl 1178 CH CH CHCH CH 4-fluorophenethyl 1179 CH CH CH CH CH 4-bromophenethyl 1180 CH CHCH CH CH 4-chlorophenethyl 1181 CH CH CH CH CH3-trifluoromethylphenethyl 1182 CH CH CH CH CH 3,4-dimethoxyphenethyl1183 CH CH CH CH CH 3-propoxyphenethyl 1184 CH CH CH CH CH3,5-difluorophenethyl 1185 CH CH CH CH CH 4-dimethylaminophenethyl 1186CH CH CH CH CH 3-difluoromethoxyphenethyl 1187 CH CH CH CH CH2-methylphenethyl 1188 CH CH CH CH CH 4-acetylphenethyl 1189 CH CH CH CHCH 4-dimethylamino-2-methoxyphenethyl 1190 CH CH CH CH CHcyclohexylethyl 1191 CH CH CH CH CH 2-(2-pyridyl)ethyl 1192 CH CH CH CHCH 2-(3-pyridyl)ethyl 1193 CH CH CH CH CH 2-(4-pyridyl)ethyl 1194 CH CHCH CH CH 2-(2-quinolyl)ethyl 1195 CH CH CH CH CH 2-(3-quinolyl)ethyl1196 CH CH CH CH CH 2-(4-quinolyl)ethyl 1197 CH CH CH CH CH2-(6-quinolyl)ethyl 1198 CH CH CH CH CH 2-(2-indolyl)ethyl 1199 CH CH CHCH CH 2-(3-indolyl)ethyl 1200 CH CH CH CH CH 2-(7-aza-3-indolyl)ethyl1201 CH CH CH CH CH 2-(benzimidazolyl)ethyl 1202 CH CH CH CH CH2-(benzoxazolyl)ethyl 1203 CH CH CH CH CH 2-(benzothiazolyl)ethyl 1204CH CH CH CH CH 2-(1-naphthyl)ethyl 1205 CH CH CH CH CH2-(2-naphthyl)ethyl 1206 CH CH CH CH CH 1-(hydroxymethyl)-2-phenylethyl1207 CH CH CH CH CH 1-(methoxycarbonyl)-2-phenylethyl 1208 CH CH CH CHCH 1-(ethoxycarbonyl)-2-phenylethyl 1209 CH CH CH CH CH1-carboxy-2-phenylethyl 1210 CH CH CH CH CH1-(benzyloxycarbonyl)-2-phenyl- ethyl 1211 CH CH CH CH CH1-(phenoxymethyl)-2-phenylethyl 1212 CH CH CH CH CH1-(benzyloxymethyl)-2-phenylethyl 1213 CH CH CH CH CH1-(benzylcarbamoyl)-2-phenylethyl 1214 CH CH CH CH CH1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1215 CH CH CH CH CH1-(phenylcarbamoyl)-2-phenylethyl 1216 CH CH CH CH CH1-(N-methylphenylcarbamoyl)-2- phenylethyl 1217 CH CH CH CH CH1-(N-benzylaminomethyl)-2-phenyl- ethyl 1218 CH CH CH CH CH1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 1219 CH CH CH CH CH1-(anilinomethyl)-2-phenylethyl 1220 CH CH CH CH CH1-(N-methylanilinomethyl)-2- phenylethyl 1221 CH CH CH CH CH1-(N-methylaminomethyl)-2- phenylethyl 1222 CH CH CH CH CH1-(N-ethylaminomethyl)-2- phenylethyl 1223 CH CH CH CH CH1-(N-isobutylaminomethyl)-2- phenylethyl 1224 CH CH CH CH CH1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1225 CH CH CH CH CH1-(aminomethyl)-2-phenylethyl 1226 CH CH CH CH CH1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1227 CH CH CH CH CH1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1228 CH CH CH CH CH1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1229 CH CH CH CH CH2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1230 CH CH CH CH CH2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1231 CH CH CH CH CH2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1232 CH CH CH CH CH2-hydroxy-2-phenylethyl 1233 CH CH CH CH CH benzoylmethyl 1234 CH CH CHCH CH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1235 CH CH CH CH CH1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 1236 CH CH CH CH CH1-(phenoxymethyl)-2-(3- indolyl)ethyl 1237 CH CH CH CH CH2-(2-methoxyphenoxy)ethyl 1238 CH CH CH CH CH1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 1239 CH CH CH CH CH1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 1240 CH CH CH CH CH1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 1241 CH CH CH CH CH1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1242 CH CH CH CH CH1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1243 CH CH CH CH CH1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1244 CH CH CH CH CH1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 1245 CH CH CH CH CH1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 1246 CH CH CH CHCH 1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1247 CH CH CH CH CH1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1248 CH CH CH CH CH1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 1249 CH CH CH CH CH1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 1250 CH CH CH CH CH2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1251 CH CH CH CH CH2-hydroxy-2-(2-quinolyl)ethyl 1252 CH CH CH CH CH2-hydroxy-2-(3-quinolyl)ethyl 1253 CH CH CH CH CH2-hydroxy-2-(4-quinolyl)ethyl 1254 CH CH CH CH CH2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1255 CH CH CH CH CH1-carboxy-2-cyclohexylethyl 1256 CH CH CH CH CH2-hydroxy-2-(6-quinolyl)ethyl 1257 CH CH CH CH CH2-(benzylamino)-2-phenylethyl 1258 CH CH CH CH CH2-amino-2-(2-naphthyl)propyl 1259 CH CH CH CH CH 2-(phenylamino)ethyl1260 CH CH CH CH CH diphenylmethyl 1261 CH CH CH CH CH 2,2-diphenylethyl1262 CH CH CH CH CH 2-phenyl-2-(2-pyridyl)ethyl 1263 CH CH CH CH CH2-phenyl-2-(3-pyridyl)ethyl 1264 CH CH CH CH CH2-phenyl-2-(4-pyridyl)ethyl 1265 CH CH CH CH CH 2-phenoxy-2-phenylethyl1266 CH CH CH CH CH 2-(benzyloxy)-2-phenylethyl 1267 CH CH CH CH N1-phenyl-3-pyrrolidinyl 1268 CH CH CH CH N1-(2-fluorophenyl)-3-pyrrolidinyl 1269 CH CH CH CH N1-(3-fluorophenyl)-3-pyrrolidinyl 1270 CH CH CH CH N1-(4-fluorophenyl)-3-pyrrolidinyl 1271 CH CH CH CH N1-(2-chlorophenyl)-3-pyrrolidinyl 1272 CH CH CH CH N1-(3-chlorophenyl)-3-pyrrolidinyl 1273 CH CH CH CH N1-(4-chlorophenyl)-3-pyrrolidinyl 1274 CH CH CH CH N1-(2-methylphenyl)-3-pyrrolidinyl 1275 CH CH CH CH N1-(3-methylphenyl)-3-pyrrolidinyl 1276 CH CH CH CH N1-(4-methylphenyl)-3-pyrrolidinyl 1277 CH CH CH CH N1-(2-methoxyphenyl)-3-pyrrolidinyl 1278 CH CH CH CH N1-(3-methoxyphenyl)-3-pyrrolidinyl 1279 CH CH CH CH N1-(4-methoxyphenyl)-3-pyrrolidinyl 1280 CH CH CH CH N1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1281 CH CH CH CH N1-(3-trifluromethylphenyl)-3- pyrrolidinyl 1282 CH CH CH CH N1-(4-trifluromethylphenyl)-3- pyrrolidinyl 1283 CH CH CH CH N1-(3,5-diflurophenyl)-3- pyrrolidinyl 1284 CH CH CH CH N1-(2-difluromethoxyphenyl)-3- pyrrolidinyl 1285 CH CH CH CH N1-(3-difluromethoxyphenyl)-3- pyrrolidinyl 1286 CH CH CH CH N1-(4-difluromethoxyphenyl)-3- pyrrolidinyl 1287 CH CH CH CH N1-(2-pyridyl)-3-pyrrolidinyl 1288 CH CH CH CH N1-(3-pyridyl)-3-pyrrolidinyl 1289 CH CH CH CH N1-(4-pyridyl)-3-pyrrolidinyl 1290 CH CH CH CH N1-(2-pyrimidinyl)-3-pyrrolidinyl 1291 CH CH CH CH N5-oxo-1-phenyl-3-pyrrolidinyl 1292 CH CH CH CH N 1-phenyl-3-piperidyl1293 CH CH CH CH N 1-(2-fluorophenyl)-3-piperidyl 1294 CH CH CH CH N1-(3-fluorophenyl)-3-piperidyl 1295 CH CH CH CH N1-(4-fluorophenyl)-3-piperidyl 1296 CH CH CH CH N1-(2-chlorophenyl)-3-piperidyl 1297 CH CH CH CH N1-(3-chlorophenyl)-3-piperidyl 1298 CH CH CH CH N1-(4-chlorophenyl)-3-piperidyl 1299 CH CH CH CH N1-(2-methylphenyl)-3-piperidyl 1300 CH CH CH CH N1-(3-methylphenyl)-3-piperidyl 1301 CH CH CH CH N1-(4-methylphenyl)-3-piperidyl 1302 CH CH CH CH N1-(2-methoxyphenyl)-3-piperidyl 1303 CH CH CH CH N1-(3-methoxyphenyl)-3-piperidyl 1304 CH CH CH CH N1-(4-methoxyphenyl)-3-piperidyl 1305 CH CH CH CH N1-(2-trifluoromethylphenyl)-3- piperidyl 1306 CH CH CH CH N1-(3-trifluoromethylphenyl)-3- piperidyl 1307 CH CH CH CH N1-(4-trifluoromethylphenyl)-3- piperidyl 1308 CH CH CH CH N1-(3,5-difluorophenyl)-3-piperidyl 1309 CH CH CH CH N1-(2-difluoromethoxyphenyl)-3- piperidyl 1310 CH CH CH CH N1-(3-difluoromethoxyphenyl)-3- piperidyl 1311 CH CH CH CH N1-(4-difluoromethoxyphenyl)-3- piperidyl 1312 CH CH CH CH N1-(2-pyridyl)-3-piperidyl 1313 CH CH CH CH N 1-(3-pyridyl)-3-piperidyl1314 CH CH CH CH N 1-(4-pyridyl)-3-piperidyl 1315 CH CH CH CH N1-phenyl-4-piperidyl 1316 CH CH CH CH N 1-(2-fluorophenyl)-4-piperidyl1317 CH CH CH CH N 1-(3-fluorophenyl)-4-piperidyl 1318 CH CH CH CH N1-(4-fluorophenyl)-4-piperidyl 1319 CH CH CH CH N1-(2-chlorophenyl)-4-piperidyl 1320 CH CH CH CH N1-(3-chlorophenyl)-4-piperidyl 1321 CH CH CH CH N1-(4-chlorophenylj-4-piperidyl 1322 CH CH CH CH N1-(2-methylphenyl)-4-piperidyl 1323 CH CH CH CH N1-(3-methylphenyl)-4-piperidyl 1324 CH CH CH CH N1-(4-methylphenyl)-4-piperidyl 1325 CH CH CH CH N1-(2-methoxyphenyl)-4-piperidyl 1326 CH CH CH CH N1-(3-methoxyphenyl)-4-piperidyl 1327 CH CH CH CH N1-(4-methoxyphenyl)-4-piperidyl 1328 CH CH CH CH N1-(2-trifluoromethylphenyl)-4- piperidyl 1329 CH CH CH CH N1-(3-trifluoromethylphenyl)-4- piperidyl 1330 CH CH CH CH N1-(4-trifluoromethylphenyl)-4- piperidyl 1331 CH CH CH CH N1-(3,5-difluorophenyl)-4- piperidyl 1332 CH CH CH CH N1-(2-difluoromethoxyphenyl)-4- piperidyl 1333 CH CH CH CH N1-(3-difluoromethoxyphenyl)-4- piperidyl 1334 CH CH CH CH N1-(4-difluoromethoxyphenyl)-4- piperidyl 1335 CH CH CH CH N1-(2-pyridyl)-4-piperidyl 1336 CH CH CH CH N 1-(3-pyridyl)-4-piperidyl1337 CH CH CH CH N 1-(4-pyridyl)-4-piperidyl 1338 CH CH CH CH N3-hydroxymethyl-1-phenyl-4- piperidyl 1339 CH CH CH CH N3-methoxycarbonyl-1-phenyl-4- piperidyl 1340 CH CH CH CH N3-ethoxycarbonyl-1-phenyl-4- piperidyl 1341 CH CH CH CH N3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1342 CH CH CH CH N4-phenylcyclohexyl 1343 CH CH CH CH N 4-(2-fluorophenyl)cyclohexyl 1344CH CH CH CH N 4-(3-fluorophenyl)cyclohexyl 1345 CH CH CH CH N4-(4-fluorophenyl)cyclohexyl 1346 CH CH CH CH N4-(2-chlorophenyl)cyclohexyl 1347 CH CH CH CH N4-(3-chlorophenyl)cyclohexyl 1348 CH CH CH CH N4-(4-chlorophenyl)cyclohexyl 1349 CH CH CH CH N4-(2-methylphenyl)cyclohexyl 1350 CH CH CH CH N4-(3-methylphenyl)cyclohexyl 1351 CH CH CH CH N4-(4-methylphenyl)cyclohexyl 1352 CH CH CH CH N4-(2-methoxyphenyl)cyclohexyl 1353 CH CH CH CH N4-(3-methoxyphenyl)cyclohexyl 1354 CH CH CH CH N4-(4-methoxyphenyl)cyclohexyl 1355 CH CH CH CH N4-(2-trifluoromethylphenyl)cyclo- hexyl 1356 CH CH CH CH N4-(3-trifluoromethylphenyl)cyclo- hexyl 1357 CH CH CH CH N4-(4-trifluoromethylphenyl)cyclo- hexyl 1358 CH CH CH CH N4-(3,5-difluorophenyl)cyclohexyl 1359 CH CH CH CH N4-(3-acetylphenyl)cyclohexyl 1360 CH CH CH CH N4-(3-cyanophenyl)cyclohexyl 1361 CH CH CH CH N4-(2-difluoromethoxyphenyl)cyclo- hexyl 1362 CH CH CH CH N4-(3-difluoromethoxyphenyl)cyclo- hexyl 1363 CH CH CH CH N4-(4-difluoromethoxyphenyl)cyclo- hexyl 1364 CH CH CH CH N4-(2-pyridyl)cyclohexyl 1365 CH CH CH CH N 4-(3-pyridyl)cyclohexyl 1366CH CH CH CH N 4-(4-pyridyl)cyclohexyl 1367 CH CH CH CH N4-(4-fluoro-3-pyridyl)cyclohexyl 1368 CH CH CH CH N4-(3-quinolyl)cyclohexyl 1369 CH CH CH CH N4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 1370 CH CH CH CH N3-phenylcyclohexyl 1371 CH CH CH CH N 3-phenylcyclopentyl 1372 CH CH CHCH N 6-phenyl-3-tetrahydropyranyl 1373 CH CH CH CH N6-(3-fluorophenyl)-3-tetrahydro- pyranyl 1374 CH CH CH CH N2-phenylcyclopropyl 1375 CH CH CH CH N 2-(2-pyridyl)cyclopropyl 1376 CHCH CH CH N 2-(3-pyridyl)cyclopropyl 1377 CH CH CH CH N2-(4-pyridyl)cyclopropyl 1378 CH CH CH CH N2-(3-fluorophenyl)cyclopropyl 1379 CH CH CH CH N 2-indanyl 1380 CH CH CHCH N 2-tetrahydronaphthyl 1381 CH CH CH CH N6-methoxy-2-tetrahydronaphthyl 1382 CH CH CH CH N benzyl 1383 CH CH CHCH N phenethyl 1384 CH CH CH CH N 3-phenylpropyl 1385 CH CH CH CH N4-phenylbutyl 1386 CH CH CH CH N 2-methoxyphenethyl 1387 CH CH CH CH N3-methoxyphenethyl 1388 CH CH CH CH N 4-methoxyphenethyl 1389 CH CH CHCH N 4-fluorophenethyl 1390 CH CH CH CH N 4-bromophenethyl 1391 CH CH CHCH N 4-chlorophenethyl 1392 CH CH CH CH N 3-trifluoromethylphenethyl1393 CH CH CH CH N 3,4-dimethoxyphenethyl 1394 CH CH CH CH N3-propoxyphenethyl 1395 CH CH CH CH N 3,5-difluorophenethyl 1396 CH CHCH CH N 4-dimethylaminophenethyl 1397 CH CH CH CH N3-difluoromethoxyphenethyl 1398 CH CH CH CH N 2-methylphenethyl 1399 CHCH CH CH N 4-acetylphenethyl 1400 CH CH CH CH N4-dimethylamino-2-methoxy- phenethyl 1401 CH CH CH CH N cyclohexylethyl1402 CH CH CH CH N 2-(2-pyridyl)ethyl 1403 CH CH CH CH N2-(3-pyridyl)ethyl 1404 CH CH CH CH N 2-(4-pyridyl)ethyl 1405 CH CH CHCH N 2-(2-quinolyl)ethyl 1406 CH CH CH CH N 2-(3-quinolyl)ethyl 1407 CHCH CH CH N 2-(4-quinolyl)ethyl 1408 CH CH CH CH N 2-(6-quinolyl)ethyl1409 CH CH CH CH N 2-(2-indolyl)ethyl 1410 CH CH CH CH N2-(3-indolyl)ethyl 1411 CH CH CH CH N 2-(7-aza-3-indolyl)ethyl 1412 CHCH CH CH N 2-(benzimidazolyl)ethyl 1413 CH CH CH CH N2-(benzoxazolyl)ethyl 1414 CH CH CH CH N 2-(benzothiazolyl)ethyl 1415 CHCH CH CH N 2-(1-naphthyl)ethyl 1416 CH CH CH CH N 2-(2-naphthyl)ethyl1417 CH CH CH CH N 1-(hydroxymethyl)-2-phenylethyl 1418 CH CH CH CH N1-(methoxycarbonyl)-2-phenyl- ethyl 1419 CH CH CH CH N1-(ethoxycarbonyl)-2-phenylethyl 1420 CH CH CH CH N1-carboxy-2-phenylethyl 1421 CH CH CH CH N1-(benzyloxycarbonyl)-2-phenyl- ethyl 1422 CH CH CH CH N1-(phenoxymethyl)-2-phenylethyl 1423 CH CH CH CH N1-(benzyloxymethyl)-2-phenylethyl 1424 CH CH CH CH N1-(benzylcarbamoyl)-2-phenylethyl 1425 CH CH CH CH N1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1426 CH CH CH CH N1-(phenylcarbamoyl)-2-phenylethyl 1427 CH CH CH CH N1-(N-methylphenylcarbamoyl)-2- phenylethyl 1428 CH CH CH CH N1-(N-benzylaminomethyl)-2- phenylethyl 1429 CH CH CH CH N1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 1430 CH CH CH CH N1-(anilinomethyl)-2-phenylethyl 1431 CH CH CH CH N1-(N-methylanilinomethyl)-2- phenylethyl 1432 CH CH CH CH N1-(N-methylaminomethyl)-2- phenylethyl 1433 CH CH CH CH N1-(N-ethylaminomethyl)-2- phenylethyl 1434 CH CH CH CH N1-(N-isobutylaminomethyl)-2- phenylethyl 1435 CH CH CH CH N1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1436 CH CH CH CH N1-(aminomethyl)-2-phenylethyl 1437 CH CH CH CH N1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1438 CH CH CH CH N1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1439 CH CH CH CH N1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1440 CH CH CH CH N2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1441 CH CH CH CH N2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1442 CH CH CH CH N2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1443 CH CH CH CH N2-hydroxy-2-phenylethyl 1444 CH CH CH CH N benzoylmethyl 1445 CH CH CHCH N 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1446 CH CH CH CH N1-(benzyloxycarbonyl)-2- cyclohexylethyl 1447 CH CH CH CH N1-(phenoxymethyl)-2-(3- indolyl)ethyl 1448 CH CH CH CH N2-(2-methoxyphenoxy)ethyl 1449 CH CH CH CH N1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 1450 CH CH CH CH N1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 1451 CH CH CH CH N1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 1452 CH CH CH CH N1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1453 CH CH CH CH N1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1454 CH CH CH CH N1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1455 CH CH CH CH N1-(benzylcarbamoyl)-2- (4-pyridyl)ethyl 1456 CH CH CH CH N1-(4-pyridylmethylcarbamoyl)-2- (4-fluorophenyl)ethyl 1457 CH CH CH CH N1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1458 CH CH CH CH N1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1459 CH CH CH CH N1-(N-benzyl-N-methylaminomethyl)-2- (3-pyridyl)ethyl 1460 CH CH CH CH N1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 1461 CH CH CH CH N2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1462 CH CH CH CH N2-hydroxy-2-(2-quinolyl)ethyl 1463 CH CH CH CH N2-hydroxy-2-(3-quinolyl)ethyl 1464 CH CH CH CH N2-hydroxy-2-(4-quinolyl)ethyl 1465 CH CH CH CH N2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1466 CH CH CH CH N1-carboxy-2-cyclohexylethyl 1467 CH CH CH CH N2-hydroxy-2-(6-quinolyl)ethyl 1468 CH CH CH CH N2-(benzylamino)-2-phenylethyl 1469 CH CH CH CH N2-amino-2-(2-naphthyl)propyl 1470 CH CH CH CH N 2-(phenylamino)ethyl1471 CH CH CH CH N diphenylmethyl 1472 CH CH CH CH N 2,2-diphenylethyl1473 CH CH CH CH N 2-phenyl-2-(2-pyridyl)ethyl 1474 CH CH CH CH N2-phenyl-2-(3-pyridyl)ethyl 1475 CH CH CH CH N2-phenyl-2-(4-pyridyl)ethyl 1476 CH CH CH CH N 2-phenoxy-2-phenylethyl1477 CH CH CH CH N 2-(benzyloxy)-2-phenylethyl 1478 N CH CH CH CH1-phenyl-3-pyrrolidinyl 1479 N CH CH CH CH1-(2-fluorophenyl)-3-pyrrolidinyl 1480 N CH CH CH CH1-(3-fluorophenyl)-3-pyrrolidinyl 1481 N CH CH CH CH1-(4-fluorophenyl)-3-pyrrolidinyl 1482 N CH CH CH CH1-(2-chlorophenyl)-3-pyrrolidinyl 1483 N CH CH CH CH1-(3-chlorophenyl)-3-pyrrolidinyl 1484 N CH CH CH CH1-(4-chlorophenyl)-3-pyrrolidinyl 1485 N CH CH CH CH1-(2-methylphenyl)-3-pyrrolidinyl 1486 N CH CH CH CH1-(3-methylphenyl)-3-pyrrolidinyl 1487 N CH CH CH CH1-(4-methylphenyl)-3-pyrrolidinyl 1488 N CH CH CH CH1-(2-methoxyphenyl)-3- pyrrolidinyl 1489 N CH CH CH CH1-(3-methoxyphenyl)-3- pyrrolidinyl 1490 N CH CH CH CH1-(4-methoxyphenyl)-3- pyrrolidinyl 1491 N CH CH CH CH1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1492 N CH CH CH CH1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1493 N CH CH CH CH1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1494 N CH CH CH CH1-(3,5-difluorophenyl)-3- pyrrolidinyl 1495 N CH CH CH CH1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1496 N CH CH CH CH1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1497 N CH CH CH CH1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1498 N CH CH CH CH1-(2-pyridyl)-3-pyrrolidinyl 1499 N CH CH CH CH1-(3-pyridyl)-3-pyrrolidinyl 1500 N CH CH CH CH1-(4-pyridyl)-3-pyrrolidinyl 1501 N CH CH CH CH1-(2-pyrimidinyl)-3-pyrrolidinyl 1502 N CH CH CH CH5-oxo-1-phenyl-3-pyrrolidinyl 1503 N CH CH CH CH 1-phenyl-3-piperidyl1504 N CH CH CH CH 1-(2-fluorophenyl)-3-piperidyl 1505 N CH CH CH CH1-(3-fluorophenyl)-3-piperidyl 1506 N CH CH CH CH1-(4-fluorophenyl)-3-piperidyl 1507 N CH CH CH CH1-(2-chlorophenyl)-3-piperidyl 1508 N CH CH CH CH1-(3-chlorophenyl)-3-piperidyl 1509 N CH CH CH CH1-(4-chlorophenyl)-3-piperidyl 1510 N CH CH CH CH1-(2-methylphenyl)-3-piperidyl 1511 N CH CH CH CH1-(3-methylphenyl)-3-piperidyl 1512 N CH CH CH CH1-(4-methylphenyl)-3-piperidyl 1513 N CH CH CH CH1-(2-methoxyphenyl)-3-piperidyl 1514 N CH CH CH CH1-(3-methoxyphenyl)-3-piperidyl 1515 N CH CH CH CH1-(4-methoxyphenyl)-3-piperidyl 1516 N CH CH CH CH1-(2-trifluoromethylphenyl)-3- piperidyl 1517 N CH CH CH CH1-(3-trifluoromethylphenyl)-3- piperidyl 1518 N CH CH CH CH1-(4-trifluoromethylphenyl)-3- piperidyl 1519 N CH CH CH CH1-(3,5-difluorophenyl)-3- piperidyl 1520 N CH CH CH CH1-(2-difluoromethoxyphenyl)-3- piperidyl 1521 N CH CH CH CH1-(3-difluoromethoxyphenyl)-3- piperidyl 1522 N CH CH CH CH1-(4-difluoromethoxyphenyl)-3- piperidyl 1523 N CH CH CH CH1-(2-pyridyl)-3-piperidyl 1524 N CH CH CH CH 1-(3-pyridyl)-3-piperidyl1525 N CH CH CH CH 1-(4-pyridyl)-3-piperidyl 1526 N CH CH CH CH1-phenyl-4-piperidyl 1527 N CH CH CH CH 1-(2-fluorophenyl)-4-piperidyl1528 N CH CH CH CH 1-(3-fluorophenyl)-4-piperidyl 1529 N CH CH CH CH1-(4-fluorophenyl)-4-piperidyl 1530 N CH CH CH CH1-(2-chlorophenyl)-4-piperidyl 1531 N CH CH CH CH1-(3-chlorophenyl)-4-piperidyl 1532 N CH CH CH CH1-(4-chlorophenyl)-4-piperidyl 1533 N CH CH CH CH1-(2-methylphenyl)-4-piperidyl 1534 N CH CH CH CH1-(3-methylphenyl)-4-piperidyl 1535 N CH CH CH CH1-(4-methylphenyl)-4-piperidyl 1536 N CH CH CH CH1-(2-methoxyphenyl)-4-piperidyl 1537 N CH CH CH CH1-(3-methoxyphenyl)-4-piperidyl 1538 N CH CH CH CH1-(4-methoxyphenyl)-4-piperidyl 1539 N CH CH CH CH1-(2-trifluoromethylphenyl)-4- piperidyl 1540 N CH CH CH CH1-(3-trifluoromethylphenyl)-4- piperidyl 1541 N CH CH CH CH1-(4-trifluoromethylphenyl)-4- piperidyl 1542 N CH CH CH CH1-(3,5-difluorophenyl)-4- piperidyl 1543 N CH CH CH CH1-(2-difluoromethoxyphenyl)-4- piperidyl 1544 N CH CH CH CH1-(3-difluoromethoxyphenyl)-4- piperidyl 1545 N CH CH CH CH1-(4-difluoromethoxyphenyl)-4- piperidyl 1546 N CH CH CH CH1-(2-pyridyl)-4-piperidyl 1547 N CH CH CH CH 1-(3-pyridyl)-4-piperidyl1548 N CH CH CH CH 1-(4-pyridyl)-4-piperidyl 1549 N CH CH CH CH3-hydroxymethyl-1-phenyl-4- piperidyl 1550 N CH CH CH CH3-methoxycarbonyl-1-phenyl-4- piperidyl 1551 N CH CH CH CH3-ethoxycarbonyl-1-phenyl-4- piperidyl 1552 N CH CH CH CH3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1553 N CH CH CH CH4-phenylcyclohexyl 1554 N CH CH CH CH 4-(2-fluorophenyl)cyclohexyl 1555N CH CH CH CH 4-(3-fluorophenyl)cyclohexyl 1556 N CH CH CH CH4-(4-fluorophenyl)cyclohexyl 1557 N CH CH CH CH4-(2-chlorophenyl)cyclohexyl 1558 N CH CH CH CH4-(3-chlorophenyl)cyclohexyl 1559 N CH CH CH CH4-(4-chlorophenyl)cyclohexyl 1560 N CH CH CH CH4-(2-methylphenyl)cyclohexyl 1561 N CH CH CH CH4-(3-methylphenyl)cyclohexyl 1562 N CH CH CH CH4-(4-methylphenyl)cyclohexyl 1563 N CH CH CH CH4-(2-methoxyphenyl)cyclohexyl 1564 N CH CH CH CH4-(3-methoxyphenyl)cyclohexyl 1565 N CH CH CH CH4-(4-methoxyphenyl)cyclohexyl 1566 N CH CH CH CH4-(2-trifluoromethylphenyl)cyclo- hexyl 1567 N CH CH CH CH4-(3-trifluoromethylphenyl)cyclo- hexyl 1568 N CH CH CH CH4-(4-trifluoromethylphenyl)cyclo- hexyl 1569 N CH CH CH CH4-(3,5-difluorophenyl)cyclohexyl 1570 N CH CH CH CH4-(3-acetylphenyl)cyclohexyl 1571 N CH CH CH CH4-(3-cyanophenyl)cyclohexyl 1572 N CH CH CH CH4-(2-difluoromethoxyphenyl)cyclo- hexyl 1573 N CH CH CH CH4-(3-difluoromethoxyphenyl)cyclo- hexyl 1574 N CH CH CH CH4-(4-difluoromethoxyphenyl)cyclo- hexyl 1575 N CH CH CH CH4-(2-pyridyl)cyclohexyl 1576 N CH CH CH CH 4-(3-pyridyl)cyclohexyl 1577N CH CH CH CH 4-(4-pyridyl)cyclohexyl 1578 N CH CH CH CH4-(4-fluoro-3-pyridyl)cyclohexyl 1579 N CH CH CH CH4-(3-quinolyl)cyclohexyl 1580 N CH CH CH CH4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 1581 N CH CH CH CH3-phenylcyclohexyl 1582 N CH CH CH CH 3-phenylcyclopentyl 1583 N CH CHCH CH 6-phenyl-3-tetrahydropyranyl 1584 N CH CH CH CH6-(3-fluorophenyl)-3-tetrahydro- pyranyl 1585 N CH CH CH CH2-phenylcyclopropyl 1586 N CH CH CH CH 2-(2-pyridyl)cyclopropyl 1587 NCH CH CH CH 2-(3-pyridyl)cyclopropyl 1588 N CH CH CH CH2-(4-pyridyl)cyclopropyl 1589 N CH CH CH CH2-(3-fluorophenyl)cyclopropyl 1590 N CH CH CH CH 2-indanyl 1591 N CH CHCH CH 2-tetrahydronaphthyl 1592 N CH CH CH CH6-methoxy-2-tetrahydronaphthyl 1593 N CH CH CH CH benzyl 1594 N CH CH CHCH phenethyl 1595 N CH CH CH CH 3-phenylpropyl 1596 N CH CH CH CH4-phenylbutyl 1597 N CH CH CH CH 2-methoxyphenethyl 1598 N CH CH CH CH3-methoxyphenethyl 1599 N CH CH CH CH 4-methoxyphenethyl 1600 N CH CH CHCH 4-fluorophenethyl 1601 N CH CH CH CH 4-bromophenethyl 1602 N CH CH CHCH 4-chlorophenethyl 1603 N CH CH CH CH 3-trifluoromethylphenethyl 1604N CH CH CH CH 3,4-dimethoxyphenethyl 1605 N CH CH CH CH3-propoxyphenethyl 1606 N CH CH CH CH 3,5-difluorophenethyl 1607 N CH CHCH CH 4-dimethylaminophenethyl 1608 N CH CH CH CH3-difluoromethoxyphenethyl 1609 N CH CH CH CH 2-methylphenethyl 1610 NCH CH CH CH 4-acetylphenethyl 1611 N CH CH CH CH4-dimethylamino-2-methoxy- phenethyl 1612 N CH CH CH CH cyclohexylethyl1613 N CH CH CH CH 2-(2-pyridyl)ethyl 1614 N CH CH CH CH2-(3-pyridyl)ethyl 1615 N CH CH CH CH 2-(4-pyridyl)ethyl 1616 N CH CH CHCH 2-(2-quinolyl)ethyl 1617 N CH CH CH CH 2-(3-quinolyl)ethyl 1618 N CHCH CH CH 2-(4-quinolyl)ethyl 1619 N CH CH CH CH 2-(6-quinolyl)ethyl 1620N CH CH CH CH 2-(2-indolyl)ethyl 1621 N CH CH CH CH 2-(3-indolyl)ethyl1622 N CH CH CH CH 2-(7-aza-3-indolyl)ethyl 1623 N CH CH CH CH2-(benzimidazolyl)ethyl 1624 N CH CH CH CH 2-(benzoxazolyl)ethyl 1625 NCH CH CH CH 2-(benzothiazolyl)ethyl 1626 N CH CH CH CH2-(1-naphthyl)ethyl 1627 N CH CH CH CH 2-(2-naphthyl)ethyl 1628 N CH CHCH CH 1-(hydroxymethyl)-2-phenylethyl 1629 N CH CH CH CH1-(methoxycarbonyl)-2-phenyl- ethyl 1630 N CH CH CH CH1-(ethoxycarbonyl)-2-phenylethyl 1631 N CH CH CH CH1-carboxy-2-phenylethyl 1632 N CH CH CH CH 1-(benzyloxycarbonyl)-2-phenylethyl 1633 N CH CH CH CH 1-(phenoxymethyl)-2-phenylethyl 1634 N CHCH CH CH 1-(benzyloxymethyl)-2-phenyl- ethyl 1635 N CH CH CH CH1-(benzylcarbamoyl)-2-phenyl- ethyl 1636 N CH CH CH CH1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1637 N CH CH CH CH1-(phenylcarbamoyl)-2-phenyl- ethyl 1638 N CH CH CH CH1-(N-methylphenylcarbamoyl)-2- phenylethyl 1639 N CH CH CH CH1-(N-benzylaminomethyl)-2- phenylethyl 1640 N CH CH CH CH1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 1641 N CH CH CH CH1-(anilinomethyl)-2-phenylethyl 1642 N CH CH CH CH1-(N-methylanilinomethyl)-2- phenylethyl 1643 N CH CH CH CH1-(N-methylaminomethyl)-2-phenyl- ethyl 1644 N CH CH CH CH1-(N-ethylaminomethyl)-2-phenyl- ethyl 1645 N CH CH CH CH1-(N-isobutylaminomethyl)-2- phenylethyl 1646 N CH CH CH CH1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1647 N CH CH CH CH1-(aminomethyl)-2-phenylethyl 1648 N CH CH CH CH1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1649 N CH CH CH CH1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1650 N CH CH CH CH1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1651 N CH CH CH CH2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1652 N CH CH CH CH2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1653 N CH CH CH CH2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1654 N CH CH CH CH2-hydroxy-2-phenylethyl 1655 N CH CH CH CH benzoylmethyl 1656 N CH CH CHCH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1657 N CH CH CH CH1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 1658 N CH CH CH CH1-(phenoxymethyl)-2-(3- indolyl)ethyl 1659 N CH CH CH CH2-(2-methoxyphenoxy)ethyl 1660 N CH CH CH CH1-(benzylcarbamoyl)-2-cyclo- hexylethyl 1661 N CH CH CH CH1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 1662 N CH CH CH CH1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 1663 N CH CH CH CH1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1664 N CH CH CH CH1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1665 N CH CH CH CH1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1666 N CH CH CH CH1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 1667 N CH CH CH CH1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 1668 N CH CH CH CH1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1669 N CH CH CH CH1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1670 N CH CH CH CH1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 1671 N CH CH CH CH1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 1672 N CH CH CH CH2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1673 N CH CH CH CH2-hydroxy-2-(2-quinolyl)ethyl 1674 N CH CH CH CH2-hydroxy-2-(3-quinolyl)ethyl 1675 N CH CH CH CH2-hydroxy-2-(4-quinolyl)ethyl 1676 N CH CH CH CH2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1677 N CH CH CH CH1-carboxy-2-cyclohexylethyl 1678 N CH CH CH CH2-hydroxy-2-(6-quinolyl)ethyl 1679 N CH CH CH CH2-(benzylamino)-2-phenylethyl 1680 N CH CH CH CH2-amino-2-(2-naphthyl)propyl 1681 N CH CH CH CH 2-(phenylamino)ethyl1682 N CH CH CH CH diphenylmethyl 1683 N CH CH CH CH 2,2-diphenylethyl1684 N CH CH CH CH 2-phenyl-2-(2-pyridyl)ethyl 1685 N CH CH CH CH2-phenyl-2-(3-pyridyl)ethyl 1686 N CH CH CH CH2-phenyl-2-(4-pyridyl)ethyl 1687 N CH CH CH CH 2-phenoxy-2-phenylethyl1688 N CH CH CH CH 2-(benzyloxy)-2-phenylethyl 1689 N CH CH CH N1-phenyl-3-pyrrolidinyl 1690 N CH CH CH N1-(2-fluorophenyl)-3-pyrrolidinyl 1691 N CH CH CH N1-(3-fluorophenyl)-3-pyrrolidinyl 1692 N CH CH CH N1-(4-fluorophenyl)-3-pyrrolidinyl 1693 N CH CH CH N1-(2-chlorophenyl)-3-pyrrolidinyl 1694 N CH CH CH N1-(3-chlorophenyl)-3-pyrrolidinyl 1695 N CH CH CH N1-(4-chlorophenyl)-3-pyrrolidinyl 1696 N CH CH CH N1-(2-methylphenyl)-3-pyrrolidinyl 1697 N CH CH CH N1-(3-methylphenyl)-3-pyrrolidinyl 1698 N CH CH CH N1-(4-methylphenyl)-3-pyrrolidinyl 1699 N CH CH CH N1-(2-methoxyphenyl)-3- pyrrolidinyl 1700 N CH CH CH N1-(3-methoxyphenyl)-3- pyrrolidinyl 1701 N CH CH CH N1-(4-methoxyphenyl)-3- pyrrolidinyl 1702 N CH CH CH N1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1703 N CH CH CH N1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1704 N CH CH CH N1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1705 N CH CH CH N1-(3,5-difluorophenyl)-3- pyrrolidinyl 1706 N CH CH CH N1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1707 N CH CH CH N1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1708 N CH CH CH N1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1709 N CH CH CH N1-(2-pyridyl)-3-pyrrolidinyl 1710 N CH CH CH N1-(3-pyridyl)-3-pyrrolidinyl 1711 N CH CH CH N1-(4-pyridyl)-3-pyrrolidinyl 1712 N CH CH CH N1-(2-pyrimidinyl)-3-pyrrolidinl 1713 N CH CH CH N5-oxo-1-phenyl-3-pyrrolidinyl 1714 N CH CH CH N 1-phenyl-3-piperidyl1715 N CH CH CH N 1-(2-fluorophenyl)-3-piperidyl 1716 N CH CH CH N1-(3-fluorophenyl)-3-piperidyl 1717 N CH CH CH N1-(4-fluorophenyl)-3-piperidyl 1718 N CH CH CH N1-(2-chlorophenyl)-3-piperidyl 1719 N CH CH CH N1-(3-chlorophenyl)-3-piperidyl 1720 N CH CH CH N1-(4-chlorophenyl)-3-piperidyl 1721 N CH CH CH N1-(2-methylphenyl)-3-piperidyl 1722 N CH CH CH N1-(3-methylphenyl)-3-piperidyl 1723 N CH CH CH N1-(4-methylphenyl)-3-piperidyl 1724 N CH CH CH N1-(2-methoxyphenyl)-3-piperidyl 1725 N CH CH CH N1-(3-methoxyphenyl)-3-piperidyl 1726 N CH CH CH N1-(4-methoxyphenyl)-3-piperidyl 1727 N CH CH CH N1-(2-trifuoromethylphenyl)-3- piperidyl 1728 N CH CH CH N1-(3-trifuoromethylphenyl)-3- piperidyl 1729 N CH CH CH N1-(4-trifuoromethylphenyl)-3- piperidyl 1730 N CH CH CH N1-(3,5-difluorophenyl)-3-piperidyl 1731 N CH CH CH N1-(2-difluoromethoxyphenyl)-3- piperidyl 1732 N CH CH CH N1-(3-difluoromethoxyphenyl)-3- piperidyl 1733 N CH CH CH N1-(4-difluoromethoxyphenyl)-3- piperidiyl 1734 N CH CH CH N1-(2-pyridyl)-3-piperidyl 1735 N CH CH CH N 1-(3-pyridyl)-3-piperidyl1736 N CH CH CH N 1-(4-pyridyl)-3-piperidyl 1737 N CH CH CH N1-phenyl-4-piperidyl 1738 N CH CH CH N 1-(2-fluorophenyl)-4-piperidyl1739 N CH CH CH N 1-(3-fluorophenyl)-4-piperidyl 1740 N CH CH CH N1-(4-fluorophenyl)-4-piperidyl 1741 N CH CH CH N1-(2-chlorophenyl)-4-piperidyl 1742 N CH CH CH N1-(3-chlorophenyl)-4-piperidyl 1743 N CH CH CH N1-(4-chlorophenyl)-4-piperidyl 1744 N CH CH CH N1-(2-methylphenyl)-4-piperidyl 1745 N CH CH CH N1-(3-methylphenyl)-4-piperidyl 1746 N CH CH CH N1-(4-methylphenyl)-4-piperidyl 1747 N CH CH CH N1-(2-methoxyphenyl)-4-piperidyl 1748 N CH CH CH N1-(3-methoxyphenyl)-4-piperidyl 1749 N CH CH CH N1-(4-methoxyphenyl)-4-piperidyl 1750 N CH CH CH N1-(2-trifluoromethylphenyl)-4- piperidyl 1751 N CH CH CH N1-(3-trifluoromethylphenyl)-4- piperidyl 1752 N CH CH CH N1-(4-trifluoromethylphenyl)-4- piperidyl 1753 N CH CH CH N1-(3,5-difluorophenyl)-4- piperidyl 1754 N CH CH CH N1-(2-difluoromethoxyphenyl)-4- piperidyl 1755 N CH CH CH N1-(3-difluoromethoxyphenyl)-4- piperidyl 1756 N CH CH CH N1-(4-difluoromethoxyphenyl)-4- piperidyl 1757 N CH CH CH N1-(2-pyridyl)-4-piperidyl 1758 N CH CH CH N 1-(3-pyridyl)-4-piperidyl1759 N CH CH CH N 1-(4-pyridyl)-4-piperidyl 1760 N CH CH CH N3-hydroxymethyl-1-phenyl-4- piperidyl 1761 N CH CH CH N3-methoxycarbonyl-1-phenyl-4- piperidyl 1762 N CH CH CH N3-ethoxycarbonyl-1-phenyl-4- piperidyl 1763 N CH CH CH N3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1764 N CH CH CH N4-phenylcyclohexyl 1765 N CH CH CH N 4-(2-fluorophenyl)cyclohexyl 1766 NCH CH CH N 4-(3-fluorophenyl)cyclohexyl 1767 N CH CH CH N4-(4-fluorophenyl)cyclohexyl 1768 N CH CH CH N4-(2-chlorophenyl)cyclohexyl 1769 N CH CH CH N4-(3-chlorophenyl)cyclohexyl 1770 N CH CH CH N4-(4-chlorophenyl)cyclohexyl 1771 N CH CH CH N4-(2-methylphenyl)cyclohexyl 1772 N CH CH CH N4-(3-methylphenyl)cyclohexyl 1773 N CH CH CH N4-(4-methylphenyl)cyclohexyl 1774 N CH CH CH N4-(2-methoxyphenyl)cyclohexyl 1775 N CH CH CH N4-(3-methoxyphenyl)cyclohexyl 1776 N CH CH CH N4-(4-methoxyphenyl)cyclohexyl 1777 N CH CH CH N4-(2-trifluoromethylphenyl)cyclo- hexyl 1778 N CH CH CH N4-(3-trifluoromethylphenyl)cyclo- hexyl 1779 N CH CH CH N4-(4-trifluoromethylphenyl)cyclo- hexyl 1780 N CH CH CH N4-(3,5-difluorophenyl)cyclohexyl 1781 N CH CH CH N4-(3-acetylphenyl)cyclohexyl 1782 N CH CH CH N4-(3-cyanophenyl)cyclohexyl 1783 N CH CH CH N4-(2-difluoromethoxyphenyl)cyclo- hexyl 1784 N CH CH CH N4-(3-difluoromethoxyphenyl)cyclo- hexyl 1785 N CH CH CH N4-(4-difluoromethoxyphenyl)cyclo- hexyl 1786 N CH CH CH N4-(2-pyridyl)cyclohexyl 1787 N CH CH CH N 4-(3-pyridyl)cyclohexyl 1788 NCH CH CH N 4-(4-pyridyl)cyclohexyl 1789 N CH CH CH N4-(4-fluoro-3-pyridyl)cyclohexyl 1790 N CH CH CH N4-(3-quinolyl)cyclohexyl 1791 N CH CH CH N 4-(3-fluorophenyl)-4-hydroxy-cyclohexyl 1792 N CH CH CH N 3-phenylcyclohexyl 1793 N CH CH CH N3-phenylcyclopentyl 1794 N CH CH CH N 6-phenyl-3-tetrahydropyranyl 1795N CH CH CH N 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 1796 N CH CH CH N2-phenylcyclopropyl 1797 N CH CH CH N 2-(2-pyridyl)cyclopropyl 1798 N CHCH CH N 2-(3-pyridyl)cyclopropyl 1799 N CH CH CH N2-(4-pyridyl)cyclopropyl 1800 N CH CH CH N 2-(3-fluorophenyl)cyclopropyl1801 N CH CH CH N 2-indanyl 1802 N CH CH CH N 2-tetrahydronaphthyl 1803N CH CH CH N 6-methoxy-2-tetrahydronaphthyl 1804 N CH CH CH N benzyl1805 N CH CH CH N phenethyl 1806 N CH CH CH N 3-phenylpropyl 1807 N CHCH CH N 4-phenylbutyl 1808 N CH CH CH N 2-methoxyphenethyl 1809 N CH CHCH N 3-methoxyphenethyl 1810 N CH CH CH N 4-methoxyphenethyl 1811 N CHCH CH N 4-fluorophenethyl 1812 N CH CH CH N 4-bromophenethyl 1813 N CHCH CH N 4-chlorophenethyl 1814 N CH CH CH N 3-trifluoromethylphenethyl1815 N CH CH CH N 3,4-dimethoxyphenethyl 1816 N CH CH CH N3-propoxyphenethyl 1817 N CH CH CH N 3,5-difluorophenethyl 1818 N CH CHCH N 4-dimethylaminophenethyl 1819 N CH CH CH N3-difluoromethoxyphenethyl 1820 N CH CH CH N 2-methylphenethyl 1821 N CHCH CH N 4-acetylphenethyl 1822 N CH CH CH N 4-dimethylamino-2-methoxy-phenethyl 1823 N CH CH CH N cyclohexylethyl 1824 N CH CH CH N2-(2-pyridyl)ethyl 1825 N CH CH CH N 2-(3-pyridyl)ethyl 1826 N CH CH CHN 2-(4-pyridyl)ethyl 1827 N CH CH CH N 2-(2-quinolyl)ethyl 1828 N CH CHCH N 2-(3-quinolyl)ethyl 1829 N CH CH CH N 2-(4-quinolyl)ethyl 1830 N CHCH CH N 2-(6-quinolyl)ethyl 1831 N CH CH CH N 2-(2-indolyl)ethyl 1832 NCH CH CH N 2-(3-indolyl)ethyl 1833 N CH CH CH N 2-(7-aza-3-indolyl)ethyl1834 N CH CH CH N 2-(benzimidazolyl)ethyl 1835 N CH CH CH N2-(benzoxazolyl)ethyl 1836 N CH CH CH N 2-(benzothiazolyl)ethyl 1837 NCH CH CH N 2-(1-naphthyl)ethyl 1838 N CH CH CH N 2-(2-naphthyl)ethyl1839 N CH CH CH N 1-(hydroxymethyl)-2-phenylethyl 1840 N CH CH CH N1-(methoxycarbonyl)-2-phenylethyl 1841 N CH CH CH N1-(ethoxycarbonyl)-2-phenylethyl 1842 N CH CH CH N1-carboxy-2-phenylethyl 1843 N CH CH CH N1-(benzyloxycarbonyl)-2-phenyl- ethyl 1844 N CH CH CH N1-(phenoxymethyl)-2-phenylethyl 1845 N CH CH CH N1-(benzyloxymethyl)-2-phenylethyl 1846 N CH CH CH N1-(benzylcarbamoyl)-2-phenylethyl 1847 N CH CH CH N1-(N-methylbenzylcarbamoyl)-2- phenylethyl 1848 N CH CH CH N1-(phenylcarbamoyl)-2-phenylethyl 1849 N CH CH CH N1-(N-methylphenylcarbamoyl)-2- phenylethyl 1850 N CH CH CH N1-(N-benzylaminomethyl)-2- phenylethyl 1851 N CH CH CH N1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 1852 N CH CH CH N1-(anilinomethyl)-2-phenylethyl 1853 N CH CH CH N1-(N-methylanilinomethyl)-2- phenylethyl 1854 N CH CH CH N1-(N-methylaminomethyl)-2- phenylethyl 1855 N CH CH CH N1-(N-ethylaminomethyl)-2- phenylethyl 1856 N CH CH CH N1-(N-isobutylaminomethyl)-2- phenylethyl 1857 N CH CH CH N1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 1858 N CH CH CH N1-(aminomethyl)-2-phenylethyl 1859 N CH CH CH N1-benzyl-2-(2-pyridylmethyl- amino)ethyl 1860 N CH CH CH N1-benzyl-2-(3-pyridylmethyl- amino)ethyl 1861 N CH CH CH N1-benzyl-2-(4-pyridylmethyl- amino)ethyl 1862 N CH CH CH N2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 1863 N CH CH CH N2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 1864 N CH CH CH N2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 1865 N CH CH CH N2-hydroxy-2-phenylethyl 1866 N CH CH CH N benzoylmethyl 1867 N CH CH CHN 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 1868 N CH CH CH N1-(benzyloxycarbonyl)-2- cyclohexylethyl 1869 N CH CH CH N1-(phenoxymethyl)-2-(3- indolyl)ethyl 1870 N CH CH CH N2-(2-methoxyphenoxy)ethyl 1871 N CH CH CH N 1-(benzylcarbamoyl)-2-cyclohexylethyl 1872 N CH CH CH N 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 1873 N CH CH CH N 1-(phenylcarbamoyl)-2- cyclohexylethyl1874 N CH CH CH N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 1875 NCH CH CH N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 1876 N CH CH CH N1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 1877 N CH CH CH N1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 1878 N CH CH CH N1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 1879 N CH CH CH N1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 1880 N CH CH CH N1-(benzyloxymethyl)-2-(2- indolyl)ethyl 1881 N CH CH CH N1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 1882 N CH CH CH N1-(N-methylbenzylcarbamoyl)-2-(3- pyridyl)ethyl 1883 N CH CH CH N2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 1884 N CH CH CH N2-hydroxy-2-(2-quinolyl)ethyl 1885 N CH CH CH N2-hydroxy-2-(3-quinolyl)ethyl 1886 N CH CH CH N2-hydroxy-2-(4-quinolyl)ethyl 1887 N CH CH CH N2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 1888 N CH CH CH N1-carboxy-2-cyclohexylethyl 1889 N CH CH CH N2-hydroxy-2-(6-quinolyl)ethyl 1890 N CH CH CH N2-(benzylamino)-2-phenylethyl 1891 N CH CH CH N2-amino-2-(2-naphthyl)propyl 1892 N CH CH CH N 2-(phenylamino)ethyl 1893N CH CH CH N diphenylmethyl 1894 N CH CH CH N 2,2-diphenylethyl 1895 NCH CH CH N 2-phenyl-2-(2-pyridyl)ethyl 1896 N CH CH CH N2-phenyl-2-(3-pyridyl)ethyl 1897 N CH CH CH N2-phenyl-2-(4-pyridyl)ethyl 1898 N CH CH CH N 2-phenoxy-2-phenylethyl1899 N CH CH CH N 2-(benzyloxy)-2-phenylethyl 1900 CH N CH CH CH1-phenyl-3-pyrrolidinyl 1901 CH N CH CH CH1-(2-fluorophenyl)-3-pyrrolidinyl 1902 CH N CH CH CH1-(3-fluorophenyl)-3-pyrrolidinyl 1903 CH N CH CH CH1-(4-fluorophenyl)-3-pyrrolidinyl 1904 CH N CH CH CH1-(2-chlorophenyl)-3-pyrrolidinyl 1905 CH N CH CH CH1-(3-chlorophenyl)-3-pyrrolidinyl 1906 CH N CH CH CH1-(4-chlorophenyl)-3-pyrrolidinyl 1907 CH N CH CH CH1-(2-methylphenyl)-3-pyrrolidinyl 1908 CH N CH CH CH1-(3-methylphenyl)-3-pyrrolidinyl 1909 CH N CH CH CH1-(4-methylphenyl)-3-pyrrolidinyl 1910 CH N CH CH CH1-(2-methoxyphenyl)-3-pyrrolidinyl 1911 CH N CH CH CH1-(3-methoxyphenyl)-3-pyrrolidinyl 1912 CH N CH CH CH1-(4-methoxyphenyl)-3-pyrrolidinyl 1913 CH N CH CH CH1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 1914 CH N CH CH CH1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 1915 CH N CH CH CH1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 1916 CH N CH CH CH1-(3,5-difluorophenyl)-3- pyrrolidinyl 1917 CH N CH CH CH1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 1918 CH N CH CH CH1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 1919 CH N CH CH CH1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 1920 CH N CH CH CH1-(2-pyridyl)-3-pyrrolidinyl 1921 CH N CH CH CH1-(3-pyridyl)-3-pyrrolidinyl 1922 CH N CH CH CH1-(4-pyridyl)-3-pyrrolidinyl 1923 CH N CH CH CH1-(2-pyrimidinyl)-3-pyrrolidinyl 1924 CH N CH CH CH5-oxo-1-phenyl-3-pyrrolidinyl 1925 CH N CH CH CH 1-phenyl-3-piperidyl1926 CH N CH CH CH 1-(2-fluorophenyl)-3-piperidyl 1927 CH N CH CH CH1-(3-fluorophenyl)-3-piperidyl 1928 CH N CH CH CH1-(4-fluorophenyl)-3-piperidyl 1929 CH N CH CH CH1-(2-chlorophenyl)-3-piperidyl 1930 CH N CH CH CH1-(3-chlorophenyl)-3-piperidyl 1931 CH N CH CH CH1-(4-chlorophenyl)-3-piperidyl 1932 CH N CH CH CH1-(2-methylphenyl)-3-piperidyl 1933 CH N CH CH CH1-(3-methylphenyl)-3-piperidyl 1934 CH N CH CH CH1-(4-methylphenyl)-3-piperidyl 1935 CH N CH CH CH1-(2-methoxyphenyl)-3-piperidyl 1936 CH N CH CH CH1-(3-methoxyphenyl)-3-piperidyl 1937 CH N CH CH CH1-(4-methoxyphenyl)-3-piperidyl 1938 CH N CH CH CH1-(2-trifluoromethylphenyl)-3- piperidyl 1939 CH N CH CH CH1-(3-trifluoromethylphenyl)-3- piperidyl 1940 CH N CH CH CH1-(4-trifluoromethylphenyl)-3- piperidyl 1941 CH N CH CH CH1-(3,5-difluorophenyl)-3- piperidyl 1942 CH N CH CH CH1-(2-difluoromethoxyphenyl)-3- piperidyl 1943 CH N CH CH CH1-(3-difluoromethoxyphenyl)-3- piperidyl 1944 CH N CH CH CH1-(4-difluoromethoxyphenyl)-3- piperidyl 1945 CH N CH CH CH1-(2-pyridyl)-3-piperidyl 1946 CH N CH CH CH 1-(3-pyridyl)-3-piperidyl1947 CH N CH CH CH 1-(4-pyridyl)-3-piperidyl 1948 CH N CH CH CH1-phenyl-4-piperidyl 1949 CH N CH CH CH 1-(2-fluorophenyl)-4-piperidyl1950 CH N CH CH CH 1-(3-fluorophenyl)-4-piperidyl 1951 CH N CH CH CH1-(4-fluorophenyl)-4-piperidyl 1952 CH N CH CH CH1-(2-chlorophenyl)-4-piperidyl 1953 CH N CH CH CH1-(3-chlorophenyl)-4-piperidyl 1954 CH N CH CH CH1-(4-chlorophenyl)-4-piperidyl 1955 CH N CH CH CH1-(2-methylphenyl)-4-piperidyl 1956 CH N CH CH CH1-(3-methylphenyl)-4-piperidyl 1957 CH N CH CH CH1-(4-methylphenyl)-4-piperidyl 1958 CH N CH CH CH1-(2-methoxyphenyl)-4-piperidyl 1959 CH N CH CH CH1-(3-methoxyphenyl)-4-piperidyl 1960 CH N CH CH CH1-(4-methoxyphenyl)-4-piperidyl 1961 CH N CH CH CH1-(2-trifluoromethylphenyl)-4- piperidyl 1962 CH N CH CH CH1-(3-trifluoromethylphenyl)-4- piperidyl 1963 CH N CH CH CH1-(4-trifluoromethylphenyl)-4- piperidyl 1964 CH N CH CH CH1-(3,5-difluorophenyl)-4-piperidyl 1965 CH N CH CH CH1-(2-difluoromethoxyphenyl)-4- piperidyl 1966 CH N CH CH CH1-(3-difluoromethoxyphenyl)-4- piperidyl 1967 CH N CH CH CH1-(4-difluoromethoxyphenyl)-4- piperidyl 1968 CH N CH CH CH1-(2-pyridyl)-4-piperidyl 1969 CH N CH CH CH 1-(3-pyridyl)-4-piperidyl1970 CH N CH CH CH 1-(4-pyridyl)-4-piperidyl 1971 CH N CH CH CH3-hydroxymethyl-1-phenyl-4- piperidyl 1972 CH N CH CH CH3-methoxycarbonyl-1-phenyl-4- piperidyl 1973 CH N CH CH CH3-ethoxycarbonyl-1-phenyl-4- piperidyl 1974 CH N CH CH CH3-isopropoxycarbonyl-1-phenyl-4- piperidyl 1975 CH N CH CH CH4-phenylcyclohexyl 1976 CH N CH CH CH 4-(2-fluorophenyl)cyclohexyl 1977CH N CH CH CH 4-(3-fluorophenyl)cyclohexyl 1978 CH N CH CH CH4-(4-fluorophenyl)cyclohexyl 1979 CH N CH CH CH4-(2-chlorophenyl)cyclohexyl 1980 CH N CH CH CH4-(3-chlorophenyl)cyclohexyl 1981 CH N CH CH CH4-(4-chlorophenyl)cyclohexyl 1982 CH N CH CH CH4-(2-methylphenyl)cyclohexyl 1983 CH N CH CH CH4-(3-methylphenyl)cyclohexyl 1984 CH N CH CH CH4-(4-methylphenyl)cyclohexyl 1985 CH N CH CH CH4-(2-methoxyphenyl)cyclohexyl 1986 CH N CH CH CH4-(3-methoxyphenyl)cyclohexyl 1987 CH N CH CH CH4-(4-methoxyphenyl)cyclohexyl 1988 CH N CH CH CH4-(2-trifluoromethylphenyl)cyclo- hexyl 1989 CH N CH CH CH4-(3-trifluoromethylphenyl)cyclo- hexyl 1990 CH N CH CH CH4-(4-trifluoromethylphenyl)cyclo- hexyl 1991 CH N CH CH CH4-(3,5-difluorophenyl)cyclohexyl 1992 CH N CH CH CH4-(3-acetylphenyl)cyclohexyl 1993 CH N CH CH CH4-(3-cyanophenyl)cyclohexyl 1994 CH N CH CH CH4-(2-difluoromethoxyphenyl)cyclo- hexyl 1995 CH N CH CH CH4-(3-difluoromethoxyphenyl)cyclo- hexyl 1996 CH N CH CH CH4-(4-difluoromethoxyphenyl)cyclo- hexyl 1997 CH N CH CH CH4-(2-pyridyl)cyclohexyl 1998 CH N CH CH CH 4-(3-pyridyl)cyclohexyl 1999CH N CH CH CH 4-(4-pyridyl)cyclohexyl 2000 CH N CH CH CH4-(4-fluoro-3-pyridyl)cyclohexyl 2001 CH N CH CH CH4-(3-quinolyl)cyclohexyl 2002 CH N CH CH CH4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 2003 CH N CH CH CH3-phenylcyclohexyl 2004 CH N CH CH CH 3-phenylcyclopentyl 2005 CH N CHCH CH 6-phenyl-3-tetrahydropyranyl 2006 CH N CH CH CH6-(3-fluorophenyl)-3-tetrahydro- pyranyl 2007 CH N CH CH CH2-phenylcyclopropyl 2008 CH N CH CH CH 2-(2-pyridyl)cyclopropyl 2009 CHN CH CH CH 2-(3-pyridyl)cyclopropyl 2010 CH N CH CH CH2-(4-pyridyl)cyclopropyl 2011 CH N CH CH CH2-(3-fluorophenyl)cyclopropyl 2012 CH N CH CH CH 2-indanyl 2013 CH N CHCH CH 2-tetrahydronaphthyl 2014 CH N CH CH CH6-methoxy-2-tetrahydronaphthyl 2015 CH N CH CH CH benzyl 2016 CH N CH CHCH phenethyl 2017 CH N CH CH CH 3-phenylpropyl 2018 CH N CH CH CH4-phenylbutyl 2019 CH N CH CH CH 2-methoxyphenethyl 2020 CH N CH CH CH3-methoxyphenethyl 2021 CH N CH CH CH 4-methoxyphenethyl 2022 CH N CH CHCH 4-fluorophenethyl 2023 CH N CH CH CH 4-bromophenethyl 2024 CH N CH CHCH 4-chlorophenethyl 2025 CH N CH CH CH 3-trifluoromethylphenethyl 2026CH N CH CH CH 3,4-dimethoxyphenethyl 2027 CH N CH CH CH3-propoxyphenethyl 2028 CH N CH CH CH 3,5-difluorophenethyl 2029 CH N CHCH CH 4-dimethylaminophenethyl 2030 CH N CH CH CH3-difluoromethoxyphenethyl 2031 CH N CH CH CH 2-methylphenethyl 2032 CHN CH CH CH 4-acetylphenethyl 2033 CH N CH CH CH4-dimethylamino-2-methoxyphenethyl 2034 CH N CH CH CH cyclohexylethyl2035 CH N CH CH CH 2-(2-pyridyl)ethyl 2036 CH N CH CH CH2-(3-pyridyl)ethyl 2037 CH N CH CH CH 2-(4-pyridyl)ethyl 2038 CH N CH CHCH 2-(2-quinolyl)ethyl 2039 CH N CH CH CH 2-(3-quinolyl)ethyl 2040 CH NCH CH CH 2-(4-quinolyl)ethyl 2041 CH N CH CH CH 2-(6-quinolyl)ethyl 2042CH N CH CH CH 2-(2-indolyl)ethyl 2043 CH N CH CH CH 2-(3-indolyl)ethyl2044 CH N CH CH CH 2-(7-aza-3-indolyl)ethyl 2045 CH N CH CH CH2-(benzimidazolyl)ethyl 2046 CH N CH CH CH 2-(benzoxazolyl)ethyl 2047 CHN CH CH CH 2-(benzothiazolyl)ethyl 2048 CH N CH CH CH2-(1-naphthyl)ethyl 2049 CH N CH CH CH 2-(2-naphthyl)ethyl 2050 CH N CHCH CH 1-(hydroxymethyl)-2-phenylethyl 2051 CH N CH CH CH1-(methoxycarbonyl)-2-phenylethyl 2052 CH N CH CH CH1-(ethoxycarbonyl)-2-phenylethyl 2053 CH N CH CH CH1-carboxy-2-phenylethyl 2054 CH N CH CH CH 1-(benzyloxycarbonyl)-2-phenylethyl 2055 CH N CH CH CH 1-(phenoxymethyl)-2-phenylethyl 2056 CH NCH CH CH 1-(benzyloxymethyl)-2-phenylethyl 2057 CH N CH CH CH1-(benzylcarbamoyl)-2-phenylethyl 2058 CH N CH CH CH1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2059 CH N CH CH CH1-(phenylcarbamoyl)-2-phenylethyl 2060 CH N CH CH CH1-(N-methylphenylcarbamoyl)-2- phenylethyl 2061 CH N CH CH CH1-(N-benzylaminomethyl)-2- phenylethyl 2062 CH N CH CH CH1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 2063 CH N CH CH CH1-(anilinomethyl)-2-phenylethyl 2064 CH N CH CH CH1-(N-methylanilinomethyl)-2- phenylethyl 2065 CH N CH CH CH1-(N-methylaminomethyl)-2- phenylethyl 2066 CH N CH CH CH1-(N-ethylaminomethyl)-2- phenylethyl 2067 CH N CH CH CH1-(N-isobutylaminomethyl)-2- phenylethyl 2068 CH N CH CH CH1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2069 CH N CH CH CH1-(aminomethyl)-2-phenylethyl 2070 CH N CH CH CH1-benzyl-2-(2-pyridylmethyl- 2-amino)ethyl 2071 CH N CH CH CH1-benzyl-2-(3-pyridylmethyl- 2-amino)ethyl 2072 CH N CH CH CH1-benzyl-2-(4-pyridylmethyl- 2-amino)ethyl 2073 CH N CH CH CH2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2074 CH N CH CH CH2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2075 CH N CH CH CH2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2076 CH N CH CH CH2-hydroxy-2-phenylethyl 2077 CH N CH CH CH benzoylmethyl 2078 CH N CH CHCH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2079 CH N CH CH CH1-(benzyloxycarbonyl)-2- cyclohexylethyl 2080 CH N CH CH CH1-(phenoxymethyl)-2-(3- indolyl)ethyl 2081 CH N CH CH CH2-(2-methoxyphenoxy)ethyl 2082 CH N CH CH CH1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 2083 CH N CH CH CH1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2084 CH N CH CH CH1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 2085 CH N CH CH CH1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2086 CH N CH CH CH1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2087 CH N CH CH CH1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2088 CH N CH CH CH1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 2089 CH N CH CH CH1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 2090 CH N CH CH CH1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2091 CH N CH CH CH1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2092 CH N CH CH CH1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2093 CH N CH CH CH1-(N-methylbenzylcarbamoyl)-2-(3- pyridyl)ethyl 2094 CH N CH CH CH2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2095 CH N CH CH CH2-hydroxy-2-(2-quinolyl)ethyl 2096 CH N CH CH CH2-hydroxy-2-(3-quinolyl)ethyl 2097 CH N CH CH CH2-hydroxy-2-(4-quinolyl)ethyl 2098 CH N CH CH CH2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2099 CH N CH CH CH1-carboxy-2-cyclohexylethyl 2100 CH N CH CH CH2-hydroxy-2-(6-quinolyl)ethyl 2101 CH N CH CH CH2-(benzylamino)-2-phenylethyl 2102 CH N CH CH CH2-amino-2-(2-naphthyl)propyl 2103 CH N CH CH CH 2-(phenylamino)ethyl2104 CH N CH CH CH diphenylmethyl 2105 CH N CH CH CH 2,2-diphenylethyl2106 CH N CH CH CH 2-phenyl-2-(2-pyridyl)ethyl 2107 CH N CH CH CH2-phenyl-2-(3-pyridyl)ethyl 2108 CH N CH CH CH2-phenyl-2-(4-pyridyl)ethyl 2109 CH N CH CH CH 2-phenoxy-2-phenylethyl2110 CH N CH CH CH 2-(benzyloxy)-2-phenylethyl 2111 CH N CH CH N1-phenyl-3-pyrrolidinyl 2112 CH N CH CH N1-(2-fluorophenyl)-3-pyrrolidinyl 2113 CH N CH CH N1-(3-fluorophenyl)-3-pyrrolidinyl 2114 CH N CH CH N1-(4-fluorophenyl)-3-pyrrolidinyl 2115 CH N CH CH N1-(2-chlorophenyl)-3-pyrrolidinyl 2116 CH N CH CH N1-(3-chlorophenyl)-3-pyrrolidinyl 2117 CH N CH CH N1-(4-chlorophenyl)-3-pyrrolidinyl 2118 CH N CH CH N1-(2-methylphenyl)-3-pyrrolidinyl 2119 CH N CH CH N1-(3-methylphenyl)-3-pyrrolidinyl 2120 CH N CH CH N1-(4-methylphenyl)-3-pyrrolidinyl 2121 CH N CH CH N1-(2-methoxyphenyl)-3-pyrrolidinyl 2122 CH N CH CH N1-(3-methoxyphenyl)-3-pyrrolidinyl 2123 CH N CH CH N1-(4-methoxyphenyl)-3-pyrrolidinyl 2124 CH N CH CH N1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2125 CH N CH CH N1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2126 CH N CH CH N1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2127 CH N CH CH N1-(3,5-difluorophenyl)-3- pyrrolidinyl 2128 CH N CH CH N1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2129 CH N CH CH N1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2130 CH N CH CH N1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2131 CH N CH CH N1-(2-pyridyl)-3-pyrrolidinyl 2132 CH N CH CH N1-(3-pyridyl)-3-pyrrolidinyl 2133 CH N CH CH N1-(4-pyridyl)-3-pyrrolidinyl 2134 CH N CH CH N1-(2-pyrimidinyl)-3-pyrrolidinyl 2135 CH N CH CH N5-oxo-1-phenyl-3-pyrrolidinyl 2136 CH N CH CH N 1-phenyl-3-piperidyl2137 CH N CH CH N 1-(2-fluorophenyl)-3-piperidyl 2138 CH N CH CH N1-(3-fluorophenyl)-3-piperidyl 2139 CH N CH CH N1-(4-fluorophenyl)-3-piperidyl 2140 CH N CH CH N1-(2-chlorophenyl)-3-piperidyl 2141 CH N CH CH N1-(3-chlorophenyl)-3-piperidyl 2142 CH N CH CH N1-(4-chlorophenyl)-3-piperidyl 2143 CH N CH CH N1-(2-methylphenyl)-3-piperidyl 2144 CH N CH CH N1-(3-methylphenyl)-3-piperidyl 2145 CH N CH CH N1-(4-methylphenyl)-3-piperidyl 2146 CH N CH CH N1-(2-methoxyphenyl)-3-piperidyl 2147 CH N CH CH N1-(3-methoxyphenyl)-3-piperidyl 2148 CH N CH CH N1-(4-methoxyphenyl)-3-piperidyl 2149 CH N CH CH N1-(2-trifluoromethylphenyl)-3- piperidyl 2150 CH N CH CH N1-(3-trifluoromethylphenyl)-3- piperidyl 2151 CH N CH CH N1-(4-trifluoromethylphenyl)-3- piperidyl 2152 CH N CH CH N1-(3,5-difluorophenyl)-3-piperidyl 2153 CH N CH CH N1-(2-difluoromethoxyphenyl)-3- piperidyl 2154 CH N CH CH N1-(3-difluoromethoxyphenyl)-3- piperidyl 2155 CH N CH CH N1-(4-difluoromethoxyphenyl)-3- piperidyl 2156 CH N CH CH N1-(2-pyridyl)-3-piperidyl 2157 CH N CH CH N 1-(3-pyridyl)-3-piperidyl2158 CH N CH CH N 1-(4-pyridyl)-3-piperidyl 2159 CH N CH CH N1-phenyl-4-piperidyl 2160 CH N CH CH N 1-(2-fluorophenyl)-4-piperidyl2161 CH N CH CH N 1-(3-fluorophenyl)-4-piperidyl 2162 CH N CH CH N1-(4-fluorophenyl)-4-piperidyl 2163 CH N CH CH N1-(2-chlorophenyl)-4-piperidyl 2164 CH N CH CH N1-(3-chlorophenyl)-4-piperidyl 2165 CH N CH CH N1-(4-chlorophenyl)-4-piperidyl 2166 CH N CH CH N1-(2-methylphenyl)-4-piperidyl 2167 CH N CH CH N1-(3-methylphenyl)-4-piperidyl 2168 CH N CH CH N1-(4-methylphenyl)-4-piperidyl 2169 CH N CH CH N1-(2-methoxyphenyl)-4-piperidyl 2170 CH N CH CH N1-(3-methoxyphenyl)-4-piperidyl 2171 CH N CH CH N1-(4-methoxyphenyl)-4-piperidyl 2172 CH N CH CH N1-(2-trifluoromethylphenyl)-4- piperidyl 2173 CH N CH CH N1-(3-trifluoromethylphenyl)-4- piperidyl 2174 CH N CH CH N1-(4-trifluoromethylphenyl)-4- piperidyl 2175 CH N CH CH N1-(3,5-difluorophenyl)-4-piperidyl 2176 CH N CH CH N1-(2-difluoromethoxyphenyl)-4- piperidyl 2177 CH N CH CH N1-(3-difluoromethoxyphenyl)-4- piperidyl 2178 CH N CH CH N1-(4-difluoromethoxyphenyl)-4- piperidyl 2179 CH N CH CH N1-(2-pyridyl)-4-piperidyl 2180 CH N CH CH N 1-(3-pyridyl)-4-piperidyl2181 CH N CH CH N 1-(4-pyridyl)-4-piperidyl 2182 CH N CH CH N3-hydroxymethyl-1-phenyl-4- piperidyl 2183 CH N CH CH N3-methoxycarbonyl-1-phenyl-4- piperidyl 2184 CH N CH CH N3-ethoxycarbonyl-1-phenyl-4- piperidyl 2185 CH N CH CH N3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2186 CH N CH CH N4-phenylcyclohexyl 2187 CH N CH CH N 4-(2-fluorophenyl)cyclohexyl 2188CH N CH CH N 4-(3-fluorophenyl)cyclohexyl 2189 CH N CH CH N4-(4-fluorophenyl)cyclohexyl 2190 CH N CH CH N4-(2-chlorophenyl)cyclohexyl 2191 CH N CH CH N4-(3-chlorophenyl)cyclohexyl 2192 CH N CH CH N4-(4-chlorophenyl)cyclohexyl 2193 CH N CH CH N4-(2-methylphenyl)cyclohexyl 2194 CH N CH CH N4-(3-methylphenyl)cyclohexyl 2195 CH N CH CH N4-(4-methylphenyl)cyclohexyl 2196 CH N CH CH N4-(2-methoxyphenyl)cyclohexyl 2197 CH N CH CH N4-(3-methoxyphenyl)cyclohexyl 2198 CH N CH CH N4-(4-methoxyphenyl)cyclohexyl 2199 CH N CH CH N4-(2-trifluoromethylphenyl)cyclo- hexyl 2200 CH N CH CH N4-(3-trifluoromethylphenyl)cyclo- hexyl 2201 CH N CH CH N4-(4-trifluoromethylphenyl)cyclo- hexyl 2202 CH N CH CH N4-(3,5-difluorophenyl)cyclohexyl 2203 CH N CH CH N4-(3-acetylphenyl)cyclohexyl 2204 CH N CH CH N4-(3-cyanophenyl)cyclohexyl 2205 CH N CH CH N4-(2-difluoromethoxyphenyl)cyclo- hexyl 2206 CH N CH CH N4-(3-difluoromethoxyphenyl)cyclo- hexyl 2207 CH N CH CH N4-(4-difluoromethoxyphenyl)cyclo- hexyl 2208 CH N CH CH N4-(2-pyridyl)cyclohexyl 2209 CH N CH CH N 4-(3-pyridyl)cyclohexyl 2210CH N CH CH N 4-(4-pyridyl)cyclohexyl 2211 CH N CH CH N4-(4-fluoro-3-pyridyl)cyclohexyl 2212 CH N CH CH N4-(3-quinolyl)cyclohexyl 2213 CH N CH CH N4-(3-fluorophenyl)-4-hydroxycyclo- hexyl 2214 CH N CH CH N3-phenylcyclohexyl 2215 CH N CH CH N 3-phenylcyclopentyl 2216 CH N CH CHN 6-phenyl-3-tetrahydropyranyl 2217 CH N CH CH N 6-(3-fluorophenyl)-3-tetrahydropyranyl 2218 CH N CH CH N 2-phenylcyclopropyl 2219 CH N CH CHN 2-(2-pyridyl)cyclopropyl 2220 CH N CH CH N 2-(3-pyridyl)cyclopropyl2221 CH N CH CH N 2-(4-pyridyl)cyclopropyl 2222 CH N CH CH N2-(3-fluorophenyl)cyclopropyl 2223 CH N CH CH N 2-indanyl 2224 CH N CHCH N 2-tetrahydronaphthyl 2225 CH N CH CH N6-methoxy-2-tetrahydronaphthyl 2226 CH N CH CH N benzyl 2227 CH N CH CHN phenethyl 2228 CH N CH CH N 3-phenylpropyl 2229 CH N CH CH N4-phenylbutyl 2230 CH N CH CH N 2-methoxyphenethyl 2231 CH N CH CH N3-methoxyphenethyl 2232 CH N CH CH N 4-methoxyphenethyl 2233 CH N CH CHN 4-fluorophenethyl 2234 CH N CH CH N 4-bromophenethyl 2235 CH N CH CH N4-chlorophenethyl 2236 CH N CH CH N 3-trifiluoromethylphenethyl 2237 CHN CH CH N 3,4-dimethoxyphenethyl 2238 CH N CH CH N 3-propoxyphenethyl2239 CH N CH CH N 3,5-difluorophenethyl 2240 CH N CH CH N4-dimethylaminophenethyl 2241 CH N CH CH N 3-difluoromethoxyphenethyl2242 CH N CH CH N 2-methylphenethyl 2243 CH N CH CH N 4-acetylphenethyl2244 CH N CH CH N 4-dimethylamino-2-methoxyphenethyl 2245 CH N CH CH Ncyclohexylethyl 2246 CH N CH CH N 2-(2-pyridyl)ethyl 2247 CH N CH CH N2-(3-pyridyl)ethyl 2248 CH N CH CH N 2-(4-pyridyl)ethyl 2249 CH N CH CHN 2-(2-quinolyl)ethyl 2250 CH N CH CH N 2-(3-quinolyl)ethyl 2251 CH N CHCH N 2-(4-quinolyl)ethyl 2252 CH N CH CH N 2-(6-quinolyl)ethyl 2253 CH NCH CH N 2-(2-indolyl)ethyl 2254 CH N CH CH N 2-(3-indolyl)ethyl 2255 CHN CH CH N 2-(7-aza-3-indolyl)ethyl 2256 CH N CH CH N2-(benzimidazolyl)ethyl 2257 CH N CH CH N 2-(benzoxazolyl)ethyl 2258 CHN CH CH N 2-(benzothiazolyl)ethyl 2259 CH N CH CH N 2-(1-naphthyl)ethyl2260 CH N CH CH N 2-(2-naphthyl)ethyl 2261 CH N CH CH N1-(hydroxymethyl)-2-phenylethyl 2262 CH N CH CH N1-(methoxycarbonyl)-2-phenylethyl 2263 CH N CH CH N1-(ethoxycarbonyl)-2-phenylethyl 2264 CH N CH CH N1-carboxy-2-phenylethyl 2265 CH N CH CH N1-(benzyloxycarbonyl)-2-phenyl- ethyl 2266 CH N CH CH N1-(phenoxymethyl)-2-phenylethyl 2267 CH N CH CH N1-(benzyloxymethyl)-2-phenylethyl 2268 CH N CH CH N1-(benzylcarbamoyl)-2-phenylethyl 2269 CH N CH CH N1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2270 CH N CH CH N1-(phenylcarbamoyl)-2-phenylethyl 2271 CH N CH CH N1-(N-methylphenylcarbamoyl)-2- phenylethyl 2272 CH N CH CH N1-(N-benzylaminomethyl)-2- phenylethyl 2273 CH N CH CH N1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 2274 CH N CH CH N1-(anilinomethyl)-2-phenylethyl 2275 CH N CH CH N1-(N-methylanilinomethyl)-2- phenylethyl 2276 CH N CH CH N1-(N-methylaminomethyl)-2- phenylethyl 2277 CH N CH CH N1-(N-ethylaminomethyl)-2- phenylethyl 2278 CH N CH CH N1-(N-isobutylaminomethyl)-2- phenylethyl 2279 CH N CH CH N1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2280 CH N CH CH N1-(aminomethyl)-2-phenylethyl 2281 CH N CH CH N1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2282 CH N CH CH N1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2283 CH N CH CH N1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2284 CH N CH CH N2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2285 CH N CH CH N2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2286 CH N CH CH N2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2287 CH N CH CH N2-hydroxy-2-phenylethyl 2288 CH N CH CH N benzoylmethyl 2289 CH N CH CHN 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2290 CH N CH CH N1-(benzyloxycarbonyl)-2- cyclohexylethyl 2291 CH N CH CH N1-(phenoxymethyl)-2-(3- indolyl)ethyl 2292 CH N CH CH N2-(2-methoxyphenoxy)ethyl 2293 CH N CH CH N 1-(benzylcarbamoyl)-2-cyclohexylethyl 2294 CH N CH CH N 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 2295 CH N CH CH N 1-(phenylcarbamoyl)-2- cyclohexylethyl2296 CH N CH CH N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2297 CHN CH CH N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2298 CH N CH CH N1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2299 CH N CH CH N1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 2300 CH N CH CH N1-(4-pyridylmethylcarbamoyl)-2- (4-fluorophenyl)ethyl 2301 CH N CH CH N1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2302 CH N CH CH N1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2303 CH N CH CH N1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2304 CH N CH CH N1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 2305 CH N CH CH N2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2306 CH N CH CH N2-hydroxy-2-(2-quinolyl)ethyl 2307 CH N CH CH N2-hydroxy-2-(3-quinolyl)ethyl 2308 CH N CH CH N2-hydroxy-2-(4-quinolyl)ethyl 2309 CH N CH CH N2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2310 CH N CH CH N1-carboxy-2-cyclohexylethyl 2311 CH N CH CH N2-hydroxy-2-(6-quinolyl)ethyl 2312 CH N CH CH N2-(benzylamino)-2-phenylethyl 2313 CH N CH CH N2-amino-2-(2-naphthyl)propyl 2314 CH N CH CH N 2-(phenylamino)ethyl 2315CH N CH CH N diphenylmethyl 2316 CH N CH CH N 2,2-diphenylethyl 2317 CHN CH CH N 2-phenyl-2-(2-pyridyl)ethyl 2318 CH N CH CH N2-phenyl-2-(3-pyridyl)ethyl 2319 CH N CH CH N2-phenyl-2-(4-pyridyl)ethyl 2320 CH N CH CH N 2-phenoxy-2-phenylethyl2321 CH N CH CH N 2-(benzyloxy)-2-phenylethyl 2322 CH CH N CH CH1-phenyl-3-pyrrolidinyl 2323 CH CH N CH CH1-(2-fluorophenyl)-3-pyrrolidinyl 2324 CH CH N CH CH1-(3-fluorophenyl)-3-pyrrolidinyl 2325 CH CH N CH CH1-(4-fluorophenyl)-3-pyrrolidinyl 2326 CH CH N CH CH1-(2-chlorophenyl)-3-pyrrolidinyl 2327 CH CH N CH CH1-(3-chlorophenyl)-3-pyrrolidinyl 2328 CH CH N CH CH1-(4-chlorophenyl)-3-pyrrolidinyl 2329 CH CH N CH CH1-(2-methylphenyl)-3-pyrrolidinyl 2330 CH CH N CH CH1-(3-methylphenyl)-3-pyrrolidinyl 2331 CH CH N CH CH1-(4-methylphenyl)-3-pyrrolidinyl 2332 CH CH N CH CH1-(2-methoxyphenyl)-3-pyrrolidinyl 2333 CH CH N CH CH1-(3-methoxyphenyl)-3-pyrrolidinyl 2334 CH CH N CH CH1-(4-methoxyphenyl)-3- pyrrolidinyl 2335 CH CH N CH CH1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2336 CH CH N CH CH1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2337 CH CH N CH CH1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2338 CH CH N CH CH1-(3,5-difluorophenyl)-3- pyrrolidinyl 2339 CH CH N CH CH1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2340 CH CH N CH CH1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2341 CH CH N CH CH1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2342 CH CH N CH CH1-(2-pyridyl)-3-pyrrolidinyl 2343 CH CH N CH CH1-(3-pyridyl)-3-pyrrolidinyl 2344 CH CH N CH CH1-(4-pyridyl)-3-pyrrolidinyl 2345 CH CH N CH CH1-(2-pyrimidinyl)-3-pyrrolidinyl 2346 CH CH N CH CH5-oxo-1-phenyl-3-pyrrolidinyl 2347 CH CH N CH CH 1-phenyl-3-piperidyl2348 CH CH N CH CH 1-(2-fluorophenyl)-3-piperidyl 2349 CH CH N CH CH1-(3-fluorophenyl)-3-piperidyl 2350 CH CH N CH CH1-(4-fluorophenyl)-3-piperidyl 2351 CH CH N CH CH1-(2-chlorophenyl)-3-piperidyl 2352 CH CH N CH CH1-(3-chlorophenyl)-3-piperidyl 2353 CH CH N CH CH1-(4-chlorophenyl)-3-piperidyl 2354 CH CH N CH CH1-(2-methylphenyl)-3-piperidyl 2355 CH CH N CH CH1-(3-methylphenyl)-3-piperidyl 2356 CH CH N CH CH1-(4-methylphenyl)-3-piperidyl 2357 CH CH N CH CH1-(2-methoxyphenyl)-3-piperidyl 2358 CH CH N CH CH1-(3-methoxyphenyl)-3-piperidyl 2359 CH CH N CH CH1-(4-methoxyphenyl)-3-piperidyl 2360 CH CH N CH CH1-(2-trifluoromethylphenyl)-3- piperidyl 2361 CH CH N CH CH1-(3-trifluoromethylphenyl)-3- piperidyl 2362 CH CH N CH CH1-(4-trifluoromethylphenyl)-3- piperidyl 2363 CH CH N CH CH1-(3,5-difluorophenyl)-3-piperidyl 2364 CH CH N CH CH1-(2-difluoromethoxyphenyl)-3- piperidyl 2365 CH CH N CH CH1-(3-difluoromethoxyphenyl)-3- piperidyl 2366 CH CH N CH CH1-(4-difluoromethoxyphenyl)-3- piperidyl 2367 CH CH N CH CH1-(2-pyridyl)-3-piperidyl 2368 CH CH N CH CH 1-(3-pyridyl)-3-piperidyl2369 CH CH N CH CH 1-(4-pyridyl)-3-piperidyl 2370 CH CH N CH CH1-phenyl-4-piperidyl 2371 CH CH N CH CH 1-(2-fluorophenyl)-4-piperidyl2372 CH CH N CH CH 1-(3-fluorophenyl)-4-piperidyl 2373 CH CH N CH CH1-(4-fluorophenyl)-4-piperidyl 2374 CH CH N CH CH1-(2-chlorophenyl)-4-piperidyl 2375 CH CH N CH CH1-(3-chlorophenyl)-4-piperidyl 2376 CH CH N CH CH1-(4-chlorophenyl)-4-piperidyl 2377 CH CH N CH CH1-(2-methylphenyl)-4-piperidyl 2378 CH CH N CH CH1-(3-methylphenyl)-4-piperidyl 2379 CH CH N CH CH1-(4-methylphenyl)-4-piperidyl 2380 CH CH N CH CH1-(2-methoxyphenyl)-4-piperidyl 2381 CH CH N CH CH1-(3-methoxyphenyl)-4-piperidyl 2382 CH CH N CH CH1-(4-methoxyphenyl)-4-piperidyl 2383 CH CH N CH CH1-(2-trifluoromethylphenyl)-4- piperidyl 2384 CH CH N CH CH1-(3-trifluoromethylphenyl)-4- piperidyl 2385 CH CH N CH CH1-(4-trifluoromethylphenyl)-4- piperidyl 2386 CH CH N CH CH1-(3,5-difluorophenyl)-4-piperidyl 2387 CH CH N CH CH1-(2-difluoromethoxyphenyl)-4- piperidyl 2388 CH CH N CH CH1-(3-difluoromethoxyphenyl)-4- piperidyl 2389 CH CH N CH CH1-(4-difluoromethoxyphenyl)-4- piperidyl 2390 CH CH N CH CH1-(2-pyridyl)-4-piperidyl 2391 CH CH N CH CH 1-(3-pyridyl)-4-piperidyl2392 CH CH N CH CH 1-(4-pyridyl)-4-piperidyl 2393 CH CH N CH CH3-hydroxymethyl-1-phenyl-4- piperidyl 2394 CH CH N CH CH3-methoxycarbonyl-1-phenyl-4- piperidyl 2395 CH CH N CH CH3-ethoxycarbonyl-1-phenyl-4- piperidyl 2396 CH CH N CH CH3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2397 CH CH N CH CH4-phenylcyclohexyl 2398 CH CH N CH CH 4-(2-fluorophenyl)cyclohexyl 2399CH CH N CH CH 4-(3-fluorophenyl)cyclohexyl 2400 CH CH N CH CH4-(4-fluorophenyl)cyclohexyl 2401 CH CH N CH CH4-(2-chlorophenyl)cyclohexyl 2402 CH CH N CH CH4-(3-chlorophenyl)cyclohexyl 2403 CH CH N CH CH4-(4-chlorophenyl)cyclohexyl 2404 CH CH N CH CH4-(2-methylphenyl)cyclohexyl 2405 CH CH N CH CH4-(3-methylphenyl)cyclohexyl 2406 CH CH N CH CH4-(4-methylphenyl)cyclohexyl 2407 CH CH N CH CH4-(2-methoxyphenyl)cyclohexyl 2408 CH CH N CH CH4-(3-methoxyphenyl)cyclohexyl 2409 CH CH N CH CH4-(4-methoxyphenyl)cyclohexyl 2410 CH CH N CH CH4-(2-trifluoromethylphenyl)cyclo- hexyl 2411 CH CH N CH CH4-(3-trifluoromethylphenyl)cyclo- hexyl 2412 CH CH N CH CH4-(4-trifluoromethylphenyl)cyclo- hexyl 2413 CH CH N CH CH4-(3,5-difluorophenyl)cyclohexyl 2414 CH CH N CH CH4-(3-acetylphenyl)cyclohexyl 2415 CH CH N CH CH4-(3-cyanophenyl)cyclohexyl 2416 CH CH N CH CH4-(2-difluoromethoxyphenyl)cyclo- hexyl 2417 CH CH N CH CH4-(3-difluoromethoxyphenyl)cyclo- hexyl 2418 CH CH N CH CH4-(4-difluoromethoxyphenyl)cyclo- hexyl 2419 CH CH N CH CH4-(2-pyridyl)cyclohexyl 2420 CH CH N CH CH 4-(3-pyridyl)cyclohexyl 2421CH CH N CH CH 4-(4-pyridyl)cyclohexyl 2422 CH CH N CH CH4-(4-fluoro-3-pyridyl)cyclohexyl 2423 CH CH N CH CH4-(3-quinolyl)cyclohexyl 2424 CH CH N CH CH4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 2425 CH CH N CH CH3-phenylcyclohexyl 2426 CH CH N CH CH 3-phenylcyclopentyl 2427 CH CH NCH CH 6-phenyl-3-tetrhydropyranyl 2428 CH CH N CH CH6-(3-fluorophenyl)-3-tetrhydro- pyranyl 2429 CH CH N CH CH2-phenylcyclopropyl 2430 CH CH N CH CH 2-(2-pyridyl)cyclopropyl 2431 CHCH N CH CH 2-(3-pyridyl)cyclopropyl 2432 CH CH N CH CH2-(4-pyridyl)cyclopropyl 2433 CH CH N CH CH2-(3-fluorophenyl)cyclopropyl 2434 CH CH N CH CH 2-indanyl 2435 CH CH NCH CH 2-tetrahydronaphthyl 2436 CH CH N CH CH6-methoxy-2-tetrahydronaphthyl 2437 CH CH N CH CH benzyl 2438 CH CH N CHCH phenethyl 2439 CH CH N CH CH 3-phenylpropyl 2440 CH CH N CH CH4-phenylbutyl 2441 CH CH N CH CH 2-methoxyphenethyl 2442 CH CH N CH CH3-methoxyphenethyl 2443 CH CH N CH CH 4-methoxyphenethyl 2444 CH CH N CHCH 4-fluorophenethyl 2445 CH CH N CH CH 4-bromophenethyl 2446 CH CH N CHCH 4-chlorophenethyl 2447 CH CH N CH CH 3-trifluoromethylphenethyl 2448CH CH N CH CH 3,4-dimethoxyphenethyl 2449 CH CH N CH CH3-propoxyphenethyl 2450 CH CH N CH CH 3,5-difluorophenethyl 2451 CH CH NCH CH 4-dimethylaminophenethyl 2452 CH CH N CH CH3-difluoromethoxyphenethyl 2453 CH CH N CH CH 2-methylphenethyl 2454 CHCH N CH CH 4-acetylphenethyl 2455 CH CH N CH CH4-dimethylamino-2-methoxyphenethyl 2456 CH CH N CH CH cyclohexylethyl2457 CH CH N CH CH 2-(2-pyridyl)ethyl 2458 CH CH N CH CH2-(3-pyridyl)ethyl 2459 CH CH N CH CH 2-(4-pyridyl)ethyl 2460 CH CH N CHCH 2-(2-quinolyl)ethyl 2461 CH CH N CH CH 2-(3-quinolyl)ethyl 2462 CH CHN CH CH 2-(4-quinolyl)ethyl 2463 CH CH N CH CH 2-(6-quinolyl)ethyl 2464CH CH N CH CH 2-(2-indolyl)ethyl 2465 CH CH N CH CH 2-(3-indolyl)ethyl2466 CH CH N CH CH 2-(7-aza-3-indolyl)ethyl 2467 CH CH N CH CH2-(benzimidazolyl)ethyl 2468 CH CH N CH CH 2-(benzoxazolyl)ethyl 2469 CHCH N CH CH 2-(benzothiazolyl)ethyl 2470 CH CH N CH CH2-(1-naphthyl)ethyl 2471 CH CH N CH CH 2-(2-naphthyl)ethyl 2472 CH CH NCH CH 1-(hydroxymethyl)-2-phenylethyl 2473 CH CH N CH CH1-(methoxycarbonyl)-2-phenylethyl 2474 CH CH N CH CH1-(ethoxycarbonyl)-2-phenylethyl 2475 CH CH N CH CH1-carboxy-2-phenylethyl 2476 CH CH N CH CH1-(benzyloxycarbonyl)-2-phenyl- ethyl 2477 CH CH N CH CH1-(phenoxymethyl)-2-phenylethyl 2478 CH CH N CH CH1-(benzyloxymethyl)-2-phenylethyl 2479 CH CH N CH CH1-(benzylcarbamoyl)-2-phenylethyl 2480 CH CH N CH CH1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2481 CH CH N CH CH1-(phenylcarbamoyl)-2-phenylethyl 2482 CH CH N CH CH1-(N-methylphenylcarbamoyl)-2- phenylethyl 2483 CH CH N CH CH1-(N-benzylaminomethyl)-2-phenyl- ethyl 2484 CH CH N CH CH1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 2485 CH CH N CH CH1-(anilinomethyl)-2-phenylethyl 2486 CH CH N CH CH1-(N-methylanilinomethyl)-2- phenylethyl 2487 CH CH N CH CH1-(N-methylaminomethyl)-2- phenylethyl 2488 CH CH N CH CH1-(N-ethylaminomethyl)-2- phenylethyl 2489 CH CH N CH CH1-(N-isobutylaminomethyl)-2- phenylethyl 2490 CH CH N CH CH1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2491 CH CH N CH CH1-(aminomethyl)-2-phenylethyl 2492 CH CH N CH CH1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2493 CH CH N CH CH1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2494 CH CH N CH CH1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2495 CH CH N CH CH2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2496 CH CH N CH CH2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2497 CH CH N CH CH2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2498 CH CH N CH CH2-hydroxy-2-phenylethyl 2499 CH CH N CH CH benzoylmethyl 2500 CH CH N CHCH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2501 CH CH N CH CH1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 2502 CH CH N CH CH1-(phenoxymethyl)-2-(3- indolyl)ethyl 2503 CH CH N CH CH2-(2-methoxyphenoxy)ethyl 2504 CH CH N CH CH1-(benzylcarbamoyl)-2-cyclohexyl- ethyl 2505 CH CH N CH CH1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2506 CH CH N CH CH1-(phenylcarbamoyl)-2-cyclohexyl- ethyl 2507 CH CH N CH CH1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2508 CH CH N CH CH1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2509 CH CH N CH CH1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2510 CH CH N CH CH1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 2511 CH CH N CH CH1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 2512 CH CH N CH CH1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2513 CH CH N CH CH1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2514 CH CH N CH CH1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2515 CH CH N CH CH1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 2516 CH CH N CH CH2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2517 CH CH N CH CH2-hydroxy-2-(2-quinolyl)ethyl 2518 CH CH N CH CH2-hydroxy-2-(3-quinolyl)ethyl 2519 CH CH N CH CH2-hydroxy-2-(4-quinolyl)ethyl 2520 CH CH N CH CH2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2521 CH CH N CH CH1-carboxy-2-cyclohexylethyl 2522 CH CH N CH CH2-hydroxy-2-(6-quinolyl)ethyl 2523 CH CH N CH CH2-(benzylamino)-2-phenylethyl 2524 CH CH N CH CH2-amino-2-(2-naphthyl)propyl 2525 CH CH N CH CH 2-(phenylamino)ethyl2526 CH CH N CH CH diphenylmethyl 2527 CH CH N CH CH 2,2-diphenylethyl2528 CH CH N CH CH 2-phenyl-2-(2-pyridyl)ethyl 2529 CH CH N CH CH2-phenyl-2-(3-pyridyl)ethyl 2530 CH CH N CH CH2-phenyl-2-(4-pyridyl)ethyl 2531 CH CH N CH CH 2-phenoxy-2-phenylethyl2532 CH CH N CH CH 2-(benzyloxy)-2-phenylethyl 2533 CH CH N CH N1-phenyl-3-pyrrolidinyl 2534 CH CH N CH N1-(2-fluorophenyl)-3-pyrrolidinyl 2535 CH CH N CH N1-(3-fluorophenyl)-3-pyrrolidinyl 2536 CH CH N CH N1-(4-fluorophenyl)-3-pyrrolidinyl 2537 CH CH N CH N1-(2-chlorophenyl)-3-pyrrolidinvl 2538 CH CH N CH N1-(3-chlorophenyl)-3-pyrrolidinyl 2539 CH CH N CH N1-(4-chlorophenyl)-3-pyrrolidinyl 2540 CH CH N CH N1-(2-methylphenyl)-3-pyrrolidinyl 2541 CH CH N CH N1-(3-methylphenyl)-3-pyrrolidinyl 2542 CH CH N CH N1-(4-methylphenyl)-3-pyrrolidinyl 2543 CH CH N CH N1-(2-methoxyphenyl)-3-pyrrolidinyl 2544 CH CH N CH N1-(3-methoxyphenyl)-3-pyrrolidinyl 2545 CH CH N CH N1-(4-methoxyphenyl)-3-pyrrolidinyl 2546 CH CH N CH N1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2547 CH CH N CH N1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2548 CH CH N CH N1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2549 CH CH N CH N1-(3,5-diflurophenyl)-3- pyrrolidinyl 2550 CH CH N CH N1-(2-difluromethoxyphenyl)-3- pyrrolidinyl 2551 CH CH N CH N1-(3-difluromethoxyphenyl)-3- pyrrolidinyl 2552 CH CH N CH N1-(4-difluromethoxyphenyl)-3- pyrrolidinyl 2553 CH CH N CH N1-(2-pyridyl)-3-pyrrolidinyl 2554 CH CH N CH N1-(3-pyridyl)-3-pyrrolidinyl 2555 CH CH N CH N1-(4-pyridyl)-3-pyrrolidinyl 2556 CH CH N CH N1-(2-pyrimidinyl)-3-pyrrolidinyl 2557 CH CH N CH N5-oxo-1-phenyl-3-pyrrolidinyl 2558 CH CH N CH N 1-phenyl-3-piperidyl2559 CH CH N CH N 1-(2-fluorophenyl)-3-piperidyl 2560 CH CH N CH N1-(3-fluorophenyl)-3-piperidyl 2561 CH CH N CH N1-(4-fluorophenyl)-3-piperidyl 2562 CH CH N CH N1-(2-chlorophenyl)-3-piperidyl 2563 CH CH N CH N1-(3-chlorophenyl)-3-piperidyl 2564 CH CH N CH N1-(4-chlorophenyl)-3-piperidyl 2565 CH CH N CH N1-(2-methylphenyl)-3-piperidyl 2566 CH CH N CH N1-(3-methylphenyl)-3-piperidyl 2567 CH CH N CH N1-(4-methylphenyl)-3-piperidyl 2568 CH CH N CH N1-(2-methoxyphenyl)-3-piperidyl 2569 CH CH N CH N1-(3-methoxyphenyl)-3-piperidyl 2570 CH CH N CH N1-(4-methoxyphenyl)-3-piperidyl 2571 CH CH N CH N1-(2-trifluoromethylphenyl)-3- piperidyl 2572 CH CH N CH N1-(3-trifluoromethylphenyl)-3- piperidyl 2573 CH CH N CH N1-(4-trifluoromethylphenyl)-3- piperidyl 2574 CH CH N CH N1-(3,5-difluorophenyl)-3-piperidyl 2575 CH CH N CH N1-(2-difluoromethoxyphenyl)-3- piperidyl 2576 CH CH N CH N1-(3-difluoromethoxyphenyl)-3- piperidyl 2577 CH CH N CH N1-(4-difluoromethoxyphenyl)-3- piperidyl 2578 CH CH N CH N1-(2-pyridyl)-3-piperidyl 2579 CH CH N CH N 1-(3-pyridyl)-3-piperidyl2580 CH CH N CH N 1-(4-pyridyl)-3-piperidyl 2581 CH CH N CH N1-phenyl-4-piperidyl 2582 CH CH N CH N 1-(2-fluorophenyl)-4-piperidyl2583 CH CH N CH N 1-(3-fluorophenyl)-4-piperidyl 2584 CH CH N CH N1-(4-fluorophenyl)-4-piperidyl 2585 CH CH N CH N1-(2-chlorophenyl)-4-piperidyl 2586 CH CH N CH N1-(3-chlorophenyl)-4-piperidyl 2587 CH CH N CH N1-(4-chlorophenyl)-4-piperidyl 2588 CH CH N CH N1-(2-methylphenyl)-4-piperidyl 2589 CH CH N CH N1-(3-methylphenyl)-4-piperidyl 2590 CH CH N CH N1-(4-methylphenyl)-4-piperidyl 2591 CH CH N CH N1-(2-methoxyphenyl)-4-piperidyl 2592 CH CH N CH N1-(3-methoxyphenyl)-4-piperidyl 2593 CH CH N CH N1-(4-methoxyphenyl)-4-piperidyl 2594 CH CH N CH N1-(2-trifluoromethylphenyl)-4- piperidyl 2595 CH CH N CH N1-(3-trifluoromethylphenyl)-4- piperidyl 2596 CH CH N CH N1-(4-trifluoromethylphenyl)-4- piperidyl 2597 CH CH N CH N1-(3,5-difluorophenyl)-4- piperidyl 2598 CH CH N CH N1-(2-difluoromethoxyphenyl)-4- piperidyl 2599 CH CH N CH N1-(3-difluoromethoxyphenyl)-4- piperidyl 2600 CH CH N CH N1-(4-difluoromethoxyphenyl)-4- piperidyl 2601 CH CH N CH N1-(2-pyridyl)-4-piperidyl 2602 CH CH N CH N 1-(3-pyridyl)-4-piperidyl2603 CH CH N CH N 1-(4-pyridyl)-4-piperidyl 2604 CH CH N CH N3-hydroxymethyl-1-phenyl-4- piperidyl 2605 CH CH N CH N3-methoxycarbonyl-1-phenyl-4- piperidyl 2606 CH CH N CH N3-ethoxycarbonyl-1-phenyl-4- piperidyl 2607 CH CH N CH N3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2608 CH CH N CH N4-phenylcyclohexyl 2609 CH CH N CH N 4-(2-fluorophenyl)cyclohexyl 2610CH CH N CH N 4-(3-fluorophenyl)cyclohexyl 2611 CH CH N CH N4-(4-fluorophenyl)cyclohexyl 2612 CH CH N CH N4-(2-chlorophenyl)cyclohexyl 2613 CH CH N CH N4-(3-chlorophenyl)cyclohexyl 2614 CH CH N CH N4-(4-chlorophenyl)cyclohexyl 2615 CH CH N CH N4-(2-methylphenyl)cyclohexyl 2616 CH CH N CH N4-(3-methylphenyl)cyclohexyl 2617 CH CH N CH N4-(4-methylphenyl)cyclohexyl 2618 CH CH N CH N4-(2-methoxyphenyl)cyclohexyl 2619 CH CH N CH N4-(3-methoxyphenyl)cyclohexyl 2620 CH CH N CH N4-(4-methoxyphenyl)cyclohexyl 2621 CH CH N CH N4-(2-trifluoromethylphenyl)cyclo- hexyl 2622 CH CH N CH N4-(3-trifluoromethylphenyl)cyclo- hexyl 2623 CH CH N CH N4-(4-trifluoromethylphenyl)cyclo- hexyl 2624 CH CH N CH N4-(3,5-difluorophenyl)cyclohexyl 2625 CH CH N CH N4-(3-acetylphenyl)cyclohexyl 2626 CH CH N CH N4-(3-cyanophenyl)cyclohexyl 2627 CH CH N CH N4-(2-difluoromethoxyphenyl)cyclo- hexyl 2628 CH CH N CH N4-(3-difluoromethoxyphenyl)cyclo- hexyl 2629 CH CH N CH N4-(4-difluoromethoxyphenyl)cyclo- hexyl 2630 CH CH N CH N4-(2-pyridyl)cyclohexyl 2631 CH CH N CH N 4-(3-pyridyl)cyclohexyl 2632CH CH N CH N 4-(4-pyridyl)cyclohexyl 2633 CH CH N CH N4-(4-fluoro-3-pyridyl)cyclohexyl 2634 CH CH N CH N4-(3-quinolyl)cyclohexyl 2635 CH CH N CH N 4-(3-fluorophenyl)-4-hydroxy-cyclohexyl 2636 CH CH N CH N 3-phenylcyclohexyl 2637 CH CH N CH N3-phenylcyclopentyl 2638 CH CH N CH N 6-phenyl-3-tetrahydropyranyl 2639CH CH N CH N 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 2640 CH CH N CH N2-phenylcyclopropyl 2641 CH CH N CH N 2-(2-pyridyl)cyclopropyl 2642 CHCH N CH N 2-(3-pyridyl)cyclopropyl 2643 CH CH N CH N2-(4-pyridyl)cyclopropyl 2644 CH CH N CH N 2-(3-fluorophenyl)cyclopropyl2645 CH CH N CH N 2-indanyl 2646 CH CH N CH N 2-tetrahydronaphthyl 2647CH CH N CH N 6-methoxy-2-tetrahydronaphthyl 2648 CH CH N CH N benzyl2649 CH CH N CH N phenethyl 2650 CH CH N CH N 3-phenylpropyl 2651 CH CHN CH N 4-phenylbutyl 2652 CH CH N CH N 2-methoxyphenethyl 2653 CH CH NCH N 3-methoxyphenethyl 2654 CH CH N CH N 4-methoxyphenethyl 2655 CH CHN CH N 4-fluorophenethyl 2656 CH CH N CH N 4-bromophenethyl 2657 CH CH NCH N 4-chlorophenethyl 2658 CH CH N CH N 3-trifluoromethylphenethyl 2659CH CH N CH N 3,4-dimethoxyphenethyl 2660 CH CH N CH N 3-propoxyphenethyl2661 CH CH N CH N 3,5-difluorophenethyl 2662 CH CH N CH N4-dimethylaminophenethyl 2663 CH CH N CH N 3-difluoromethoxyphenethyl2664 CH CH N CH N 2-methylphenethyl 2665 CH CH N CH N 4-acetylphenethyl2666 CH CH N CH N 4-dimethylamino-2-methoxyphenethyl 2667 CH CH N CH Ncyclohexylethyl 2668 CH CH N CH N 2-(2-pyridyl)ethyl 2669 CH CH N CH N2-(3-pyridyl)ethyl 2670 CH CH N CH N 2-(4-pyridyl)ethyl 2671 CH CH N CHN 2-(2-quinolyl)ethyl 2672 CH CH N CH N 2-(3-quinolyl)ethyl 2673 CH CH NCH N 2-(4-quinolyl)ethyl 2674 CH CH N CH N 2-(6-quinolyl)ethyl 2675 CHCH N CH N 2-(2-indolyl)ethyl 2676 CH CH N CH N 2-(3-indolyl)ethyl 2677CH CH N CH N 2-(7-aza-3-indolyl)ethyl 2678 CH CH N CH N2-(benzimidazolyl)ethyl 2679 CH CH N CH N 2-(benzoxazolyl)ethyl 2680 CHCH N CH N 2-(benzothiazolyl)ethyl 2681 CH CH N CH N 2-(1-naphthyl)ethyl2682 CH CH N CH N 2-(2-naphthyl)ethyl 2683 CH CH N CH N1-(hydroxymethyl)-2-phenylethyl 2684 CH CH N CH N1-(methoxycarbonyl)-2-phenylethyl 2685 CH CH N CH N1-(ethoxycarbonyl)-2-phenylethyl 2686 CH CH N CH N1-carboxy-2-phenylethyl 2687 CH CH N CH N1-(benzyloxycarbonyl)-2-phenyl- ethyl 2688 CH CH N CH N1-(phenoxymethyl)-2-phenylethyl 2689 CH CH N CH N1-(benzyloxymethyl)-2-phenylethyl 2690 CH CH N CH N1-(benzylcarbamoyl)-2-phenylethyl 2691 CH CH N CH N1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2692 CH CH N CH N1-(phenylcarbamoyl)-2-phenylethyl 2693 CH CH N CH N1-(N-methylphenylcarbamoyl)-2- phenylethyl 2694 CH CH N CH N1-(N-benzylaminomethyl)-2- phenylethyl 2695 CH CH N CH N1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 2696 CH CH N CH N1-(anilinomethyl)-2-phenylethyl 2697 CH CH N CH N1-(N-methylanilinomethyl)-2- phenylethyl 2698 CH CH N CH N1-(N-methylaminomethyl)-2- phenylethyl 2699 CH CH N CH N1-(N-ethylaminomethyl)-2- phenylethyl 2700 CH CH N CH N1-(N-isobutylaminomethyl)-2- phenylethyl 2701 CH CH N CH N1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2702 CH CH N CH N1-(aminomethyl)-2-phenylethyl 2703 CH CH N CH N1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2704 CH CH N CH N1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2705 CH CH N CH N1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2706 CH CH N CH N2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2707 CH CH N CH N2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2708 CH CH N CH N2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2709 CH CH N CH N2-hydroxy-2-phenylethyl 2710 CH CH N CH N benzoylmethyl 2711 CH CH N CHN 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2712 CH CH N CH N1-(benzyloxycarbonyl)-2- cyclohexylethyl 2713 CH CH N CH N1-(phenoxymethyl)-2-(3- indolyl)ethyl 2714 CH CH N CH N2-(2-methoxyphenoxy)ethyl 2715 CH CH N CH N 1-(benzylcarbamoyl)-2-cyclohexylethyl 2716 CH CH N CH N 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 2717 CH CH N CH N 1-(phenylcarbamoyl)-2-cyclohexyl-ethyl 2718 CH CH N CH N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl2719 CH CH N CH N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2720 CH CH NCH N 1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2721 CH CH N CH N1-(benzylcarbamoyl)-2- 4-pyridyl)ethyl 2722 CH CH N CH N1-(4-pyridylmethylcarbamoyl)-2- (4-fluorophenyl)ethyl 2723 CH CH N CH N1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2724 CH CH N CH N1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2725 CH CH N CH N1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2726 CH CH N CH N1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 2727 CH CH N CH N2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2728 CH CH N CH N2-hydroxy-2-(2-quinolyl)ethyl 2729 CH CH N CH N2-hydroxy-2-(3-quinolyl)ethyl 2730 CH CH N CH N2-hydroxy-2-(4-quinolyl)ethyl 2731 CH CH N CH N2-hydroxy-2-(3,5-difluorophenyl) ethyl 2732 CH CH N CH N1-carboxy-2-cyclohexylethyl 2733 CH CH N CH N2-hydroxy-2-(6-quinolyl)ethyl 2734 CH CH N CH N2-(benzylamino)-2-phenylethyl 2735 CH CH N CH N2-amino-2-(2-naphthyl)propyl 2736 CH CH N CH N 2-(phenylamino)ethyl 2737CH CH N CH N diphenylmethyl 2738 CH CH N CH N 2,2-diphenylethyl 2739 CHCH N CH N 2-phenyl-2-(2-pyridyl)ethyl 2740 CH CH N CH N2-phenyl-2-(3-pyridyl)ethyl 2741 CH CH N CH N2-phenyl-2-(4-pyridyl)ethyl 2742 CH CH N CH N 2-phenoxy-2-phenylethyl2743 CH CH N CH N 2-(benzyloxy)-2-phenylethyl 2744 CH CH CH N CH1-phenyl-3-pyrrolidinyl 2745 CH CH CH N CH1-(2-fluorophenyl)-3-pyrrolidinyl 2746 CH CH CH N CH1-(3-fluorophenyl)-3-pyrrolidinyl 2747 CH CH CH N CH1-(4-fluorophenyl)-3-pyrrolidinyl 2748 CH CH CH N CH1-(2-chlorophenyl)-3-pyrrolidinyl 2749 CH CH CH N CH1-(3-chlorophenyl)-3-pyrrolidinyl 2750 CH CH CH N CH1-(4-chlorophenyl)-3-pyrrolidinyl 2751 CH CH CH N CH1-(2-methylphenyl)-3-pyrrolidinyl 2752 CH CH CH N CH1-(3-methylphenyl)-3-pyrrolidinyl 2753 CH CH CH N CH1-(4-methylphenyl)-3-pyrrolidinyl 2754 CH CH CH N CH1-(2-methoxyphenyl)-3- pyrrolidinyl 2755 CH CH CH N CH1-(3-methoxyphenyl)-3- pyrrolidinyl 2756 CH CH CH N CH1-(4-methoxyphenyl)-3- pyrrolidinyl 2757 CH CH CH N CH1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2758 CH CH CH N CH1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2759 CH CH CH N CH1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2760 CH CH CH N CH1-(3,5-difluorophenyl)-3- pyrrolidinyl 2761 CH CH CH N CH1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2762 CH CH CH N CH1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2763 CH CH CH N CH1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2764 CH CH CH N CH1-(2-pyridyl)-3-pyrrolidinyl 2765 CH CH CH N CH1-(3-pyridyl)-3-pyrrolidinyl 2766 CH CH CH N CH1-(4-pyridyl)-3-pyrrolidinyl 2767 CH CH CH N CH1-(2-pyrimidinyl)-3-pyrrolidinyl 2768 CH CH CH N CH5-oxo-1-phenyl-3-pyrrolidinyl 2769 CH CH CH N CH 1-phenyl-3-piperidyl2770 CH CH CH N CH 1-(2-fluorophenyl)-3-piperidyl 2771 CH CH CH N CH1-(3-fluorophenyl)-3-piperidyl 2772 CH CH CH N CH1-(4-fluorophenyl)-3-piperidyl 2773 CH CH CH N CH1-(2-chlorophenyl)-3-piperidyl 2774 CH CH CH N CH1-(3-chlorophenyl)-3-piperidyl 2775 CH CH CH N CH1-(4-chlorophenyl)-3-piperidyl 2776 CH CH CH N CH1-(2-methylphenyl)-3-piperidyl 2777 CH CH CH N CH1-(3-methylphenyl)-3-piperidyl 2778 CH CH CH N CH1-(4-methylphenyl)-3-piperidyl 2779 CH CH CH N CH1-(2-methoxyphenyl)-3-piperidyl 2780 CH CH CH N CH1-(3-methoxyphenyl)-3-piperidyl 2781 CH CH CH N CH1-(4-methoxyphenyl)-3-piperidyl 2782 CH CH CH N CH1-(2-trifluoromethylphenyl)-3- piperidyl 2783 CH CH CH N CH1-(3-trifluoromethylphenyl)-3- piperidyl 2784 CH CH CH N CH1-(4-trifluoromethylphenyl)-3- piperidyl 2785 CH CH CH N CH1-(3,5-difluorophenyl)-3- piperidyl 2786 CH CH CH N CH1-(2-difluoromethoxyphenyl)-3- piperidyl 2787 CH CH CH N CH1-(3-difluoromethoxyphenyl)-3- piperidyl 2788 CH CH CH N CH1-(4-difluoromethoxyphenyl)-3- piperidyl 2789 CH CH CH N CH1-(2-pyridyl)-3-piperidyl 2790 CH CH CH N CH 1-(3-pyridyl)-3-piperidyl2791 CH CH CH N CH 1-(4-pyridyl)-3-piperidyl 2792 CH CH CH N CH1-phenyl-4-piperidyl 2793 CH CH CH N CH 1-(2-fluorophenyl)-4-piperidyl2794 CH CH CH N CH 1-(3-fluorophenyl)-4-piperidyl 2795 CH CH CH N CH1-(4-fluorophenyl)-4-piperidyl 2796 CH CH CH N CH1-(2-chlorophenyl)-4-piperidyl 2797 CH CH CH N CH1-(3-chlorophenyl)-4-piperidyl 2798 CH CH CH N CH1-(4-chlorophenyl)-4-piperidyl 2799 CH CH CH N CH1-(2-methylphenyl)-4-piperidyl 2800 CH CH CH N CH1-(3-methylphenyl)-4-piperidyl 2801 CH CH CH N CH1-(4-methylphenyl)-4-piperidyl 2802 CH CH CH N CH1-(2-methoxyphenyl)-4-piperidyl 2803 CH CH CH N CH1-(3-methoxyphenyl)-4-piperidyl 2804 CH CH CH N CH1-(4-methoxyphenyl)-4-piperidyl 2805 CH CH CH N CH1-(2-trifluoromethylphenyl)-4- piperidyl 2806 CH CH CH N CH1-(3-trifluoromethylphenyl)-4- piperidyl 2807 CH CH CH N CH1-(4-trifluoromethylphenyl)-4- piperidyl 2808 CH CH CH N CH1-(3,5-difluorophenyl)-4- piperidyl 2809 CH CH CH N CH1-(2-difluoromethoxyphenyl)-4- piperidyl 2810 CH CH CH N CH1-(3-difluoromethoxyphenyl)-4- piperidyl 2811 CH CH CH N CH1-(4-difluoromethoxyphenyl)-4- piperidyl 2812 CH CH CH N CH1-(2-pyridyl)-4-piperidyl 2813 CH CH CH N CH 1-(3-pyridyl)-4-piperidyl2814 CH CH CH N CH 1-(4-pyridyl)-4-piperidyl 2815 CH CH CH N CH3-hydroxymethyl-1-phenyl-4- piperidyl 2816 CH CH CH N CH3-methoxycarbonyl-1-phenyl-4- piperidyl 2817 CH CH CH N CH3-ethoxycarbonyl-1-phenyl-4- piperidyl 2818 CH CH CH N CH3-isopropoxycarbonyl-1-phenyl-4- piperidyl 2819 CH CH CH N CH4-phenylcyclohexyl 2820 CH CH CH N CH 4-(2-fluorophenyl)cyclohexyl 2821CH CH CH N CH 4-(3-fluorophenyl)cyclohexyl 2822 CH CH CH N CH4-(4-fluorophenyl)cyclohexyl 2823 CH CH CH N CH4-(2-chlorophenyl)cyclohexyl 2824 CH CH CH N CH4-(3-chlorophenyl)cyclohexyl 2825 CH CH CH N CH4-(4-chlorophenyl)cyclohexyl 2826 CH CH CH N CH4-(2-methylphenyl)cyclohexyl 2827 CH CH CH N CH4-(3-methylphenyl)cyclohexyl 2828 CH CH CH N CH4-(4-methylphenyl)cyclohexyl 2829 CH CH CH N CH4-(2-methoxyphenyl)cyclohexyl 2830 CH CH CH N CH4-(3-methoxyphenyl)cyclohexyl 2831 CH CH CH N CH4-(4-methoxyphenyl)cyclohexyl 2832 CH CH CH N CH4-(2-trifluoromethylphenyl)cyclo- hexyl 2833 CH CH CH N CH4-(3-trifluoromethylphenyl)cyclo- hexyl 2834 CH CH CH N CH4-(4-trifluoromethylphenyl)cyclo- hexyl 2835 CH CH CH N CH4-(3,5-difluorophenyl)cyclohexyl 2836 CH CH CH N CH4-(3-acetylphenyl)cyclohexyl 2837 CH CH CH N CH4-(3-cyanophenyl)cyclohexyl 2838 CH CH CH N CH4-(2-difluoromethoxyphenyl)cyclo- hexyl 2839 CH CH CH N CH4-(3-difluoromethoxyphenyl)cyclo- hexyl 2840 CH CH CH N CH4-(4-difluoromethoxyphenyl)cyclo- hexyl 2841 CH CH CH N CH4-(2-pyridyl)cyclohexyl 2842 CH CH CH N CH 4-(3-pyridyl)cyclohexyl 2843CH CH CH N CH 4-(4-pyridyl)cyclohexyl 2844 CH CH CH N CH4-(4-fluoro-3-pyridyl)cyclohexyl 2845 CH CH CH N CH4-(3-quinolyl)cyclohexyl 2846 CH CH CH N CH4-(3-fluorophenyl)-4-hydroxy- cyclohexyl 2847 CH CH CH N CH3-phenylcyclohexyl 2848 CH CH CH N CH 3-phenylcyclopentyl 2849 CH CH CHN CH 6-phenyl-3-tetrahydropyranyl 2850 CH CH CH N CH6-(3-fluorophenyl)-3-tetrahydro- pyranyl 2851 CH CH CH N CH2-phenylcyclopropyl 2852 CH CH CH N CH 2-(2-pyridyl)cyclopropyl 2853 CHCH CH N CH 2-(3-pyridyl)cyclopropyl 2854 CH CH CH N CH2-(4-pyridyl)cyclopropyl 2855 CH CH CH N CH2-(3-fluorophenyl)cyclopropyl 2856 CH CH CH N CH 2-indanyl 2857 CH CH CHN CH 2-tetrahydronaphthyl 2858 CH CH CH N CH6-methoxy-2-tetrahydronaphthyl 2859 CH CH CH N CH benzyl 2860 CH CH CH NCH phenethyl 2861 CH CH CH N CH 3-phenylpropyl 2862 CH CH CH N CH4-phenylbutyl 2863 CH CH CH N CH 2-methoxyphenethyl 2864 CH CH CH N CH3-methoxyphenethyl 2865 CH CH CH N CH 4-methoxyphenethyl 2866 CH CH CH NCH 4-fluorophenethyl 2867 CH CH CH N CH 4-bromophenethyl 2868 CH CH CH NCH 4-chlorophenethyl 2869 CH CH CH N CH 3-trifluoromethylphenethyl 2870CH CH CH N CH 3,4-dimethoxyphenethyl 2871 CH CH CH N CH3-propoxyphenethyl 2872 CH CH CH N CH 3,5-difluorophenethyl 2873 CH CHCH N CH 4-dimethylaminophenethyl 2874 CH CH CH N CH3-difluoromethoxyphenethyl 2875 CH CH CH N CH 2-methylphenethyl 2876 CHCH CH N CH 4-acetylphenethyl 2877 CH CH CH N CH4-dimethylamino-2-methoxy- phenethyl 2878 CH CH CH N CH cyclohexylethyl2879 CH CH CH N CH 2-(2-pyridyl)ethyl 2880 CH CH CH N CH2-(3-pyridyl)ethyl 2881 CH CH CH N CH 2-(4-pyridyl)ethyl 2882 CH CH CH NCH 2-(2-quinolyl)ethyl 2883 CH CH CH N CH 2-(3-quinolyl)ethyl 2884 CH CHCH N CH 2-(4-quinolyl)ethyl 2885 CH CH CH N CH 2-(6-quinolyl)ethyl 2886CH CH CH N CH 2-(2-indolyl)ethyl 2887 CH CH CH N CH 2-(3-indolyl)ethyl2888 CH CH CH N CH 2-(7-aza-3-indolyl)ethyl 2889 CH CH CH N CH2-(benzimidazolyl)ethyl 2890 CH CH CH N CH 2-(benzoxazolyl)ethyl 2891 CHCH CH N CH 2-(benzothiazolyl)ethyl 2892 CH CH CH N CH2-(1-naphthyl)ethyl 2893 CH CH CH N CH 2-(2-naphthyl)ethyl 2894 CH CH CHN CH 1-(hydroxymethyl)-2-phenylethyl 2895 CH CH CH N CH1-(methoxycarbonyl)-2-phenylethyl 2896 CH CH CH N CH1-(ethoxycarbonyl)-2-phenylethyl 2897 CH CH CH N CH1-carboxy-2-phenylethyl 2898 CH CH CH N CH 1-(benzyloxycarbonyl)-2-phenylethyl 2899 CH CH CH N CH 1-(phenoxymethyl)-2-phenylethyl 2900 CHCH CH N CH 1-(benzyloxymethyl)-2-phenyl- ethyl 2901 CH CH CH N CH1-(benzylcarbamoyl)-2-phenylethyl 2902 CH CH CH N CH1-(N-methylbenzylcarbamoyl)-2- phenylethyl 2903 CH CH CH N CH1-(phenylcarbamoyl)-2-phenyl- ethyl 2904 CH CH CH N CH1-(N-methylphenylcarbamoyl)-2- phenylethyl 2905 CH CH CH N CH1-(N-benzylaminomethyl)-2- phenylethyl 2906 CH CH CH N CH1-(N-benzyl-N-methylamino- methyl)-2-phenylethyl 2907 CH CH CH N CH1-(anilinomethyl)-2-phenylethyl 2908 CH CH CH N CH1-(N-methylanilinomethyl)-2- phenylethyl 2909 CH CH CH N CH1-(N-methylaminomethyl)-2-phenyl- ethyl 2910 CH CH CH N CH1-(N-ethylaminomethyl)-2-phenyl- ethyl 2911 CH CH CH N CH1-(N-isobutylaminomethyl)-2- phenylethyl 2912 CH CH CH N CH1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 2913 CH CH CH N CH1-(aminomethyl)-2-phenylethyl 2914 CH CH CH N CH1-benzyl-2-(2-pyridylmethyl- amino)ethyl 2915 CH CH CH N CH1-benzyl-2-(3-pyridylmethyl- amino)ethyl 2916 CH CH CH N CH1-benzyl-2-(4-pyridylmethyl- amino)ethyl 2917 CH CH CH N CH2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 2918 CH CH CH N CH2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 2919 CH CH CH N CH2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 2920 CH CH CH N CH2-hydroxy-2-phenylethyl 2921 CH CH CH N CH benzoylmethyl 2922 CH CH CH NCH 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 2923 CH CH CH N CH1-(benzyloxycarbonyl)-2-cyclo- hexylethyl 2924 CH CH CH N CH1-(phenoxymethyl)-2-(3- indolyl)ethyl 2925 CH CH CH N CH2-(2-methoxyphenoxy)ethyl 2926 CH CH CH N CH1-(benzylcarbamoyl)-2-cyclo- hexylethyl 2927 CH CH CH N CH1-(N-methylbenzylcarbamoyl)-2- cyclohexylethyl 2928 CH CH CH N CH1-(phenylcarbamoyl)-2- cyclohexylethyl 2929 CH CH CH N CH1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 2930 CH CH CH N CH1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 2931 CH CH CH N CH1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 2932 CH CH CH N CH1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 2933 CH CH CH N CH1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 2934 CH CH CH N CH1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 2935 CH CH CH N CH1-(benzyloxymethyl)-2-(2- indolyl)ethyl 2936 CH CH CH N CH1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 2937 CH CH CH N CH1-(N-methylbenzylcarbamoyl)-2- (3-pyridyl)ethyl 2938 CH CH CH N CH2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 2939 CH CH CH N CH2-hydroxy-2-(2-quinolyl)ethyl 2940 CH CH CH N CH2-hydroxy-2-(3-quinolyl)ethyl 2941 CH CH CH N CH2-hydroxy-2-(4-quinolyl)ethyl 2942 CH CH CH N CH2-hydroxy-2-(3,5-difluoro- phenyl)ethyl 2943 CH CH CH N CH1-carboxy-2-cyclohexylethyl 2944 CH CH CH N CH2-hydroxy-2-(6-quinolyl)ethyl 2945 CH CH CH N CH2-(benzylamino)-2-phenylethyl 2946 CH CH CH N CH2-amino-2-(2-naphthyl)propyl 2947 CH CH CH N CH 2-(phenylamino)ethyl2948 CH CH CH N CH diphenylmethyl 2949 CH CH CH N CH 2,2-diphenylethyl2950 CH CH CH N CH 2-phenyl-2-(2-pyridyl)ethyl 2951 CH CH CH N CH2-phenyl-2-(3-pyridyl)ethyl 2952 CH CH CH N CH2-phenyl-2-(4-pyridyl)ethyl 2953 CH CH CH N CH 2-phenoxy-2-phenylethyl2954 CH CH CH N CH 2-(benzyloxy)-2-phenylethyl 2955 CH CH CH N N1-phenyl-3-pyrrolidinyl 2956 CH CH CH N N1-(2-fluorophenyl)-3-pyrrolidinyl 2957 CH CH CH N N1-(3-fluorophenyl)-3-pyrrolidinyl 2958 CH CH CH N N1-(4-fluorophenyl)-3-pyrrolidinyl 2959 CH CH CH N N1-(2-chlorophenyl)-3-pyrrolidinyl 2960 CH CH CH N N1-(3-chlorophenyl)-3-pyrrolidinyl 2961 CH CH CH N N1-(4-chlorophenyl)-3-pyrrolidinyl 2962 CH CH CH N N1-(2-methylphenyl)-3-pyrrolidinyl 2963 CH CH CH N N1-(3-methylphenyl)-3-pyrrolidinyl 2964 CH CH CH N N1-(4-methylphenyl)-3-pyrrolidinyl 2965 CH CH CH N N1-(2-methoxyphenyl)-3-pyrrolidinyl 2966 CH CH CH N N1-(3-methoxyphenyl)-3-pyrrolidinyl 2967 CH CH CH N N1-(4-methoxyphenyl)-3-pyrrolidinyl 2968 CH CH CH N N1-(2-trifluoromethylphenyl)-3- pyrrolidinyl 2969 CH CH CH N N1-(3-trifluoromethylphenyl)-3- pyrrolidinyl 2970 CH CH CH N N1-(4-trifluoromethylphenyl)-3- pyrrolidinyl 2971 CH CH CH N N1-(3,5-difluorophenyl)-3- pyrrolidinyl 2972 CH CH CH N N1-(2-difluoromethoxyphenyl)-3- pyrrolidinyl 2973 CH CH CH N N1-(3-difluoromethoxyphenyl)-3- pyrrolidinyl 2974 CH CH CH N N1-(4-difluoromethoxyphenyl)-3- pyrrolidinyl 2975 CH CH CH N N1-(2-pyridyl)-3-pyrrolidinyl 2976 CH CH CH N N1-(3-pyridyl)-3-pyrrolidinyl 2977 CH CH CH N N1-(4-pyridyl)-3-pyrrolidinyl 2978 CH CH CH N N1-(2-pyrimidinyl)-3-pyrrolidinyl 2979 CH CH CH N N5-oxo-1-phenyl-3-pyrrolidinyl 2980 CH CH CH N N 1-phenyl-3-piperidyl2981 CH CH CH N N 1-(2-fluorophenyl)-3-piperidyl 2982 CH CH CH N N1-(3-fluorophenyl)-3-piperidyl 2983 CH CH CH N N1-(4-fluorophenyl)-3-piperidyl 2984 CH CH CH N N1-(2-chlorophenyl)-3-piperidyl 2985 CH CH CH N N1-(3-chlorophenyl)-3-piperidyl 2986 CH CH CH N N1-(4-chlorophenyl)-3-piperidyl 2987 CH CH CH N N1-(2-methylphenyl)-3-piperidyl 2988 CH CH CH N N1-(3-methylphenyl)-3-piperidyl 2989 CH CH CH N N1-(4-methylphenyl)-3-piperidyl 2990 CH CH CH N N1-(2-methoxyphenyl)-3-piperidyl 2991 CH CH CH N N1-(3-methoxyphenyl)-3-piperidyl 2992 CH CH CH N N1-(4-methoxyphenyl)-3-piperidyl 2993 CH CH CH N N1-(2-trifuoromethylphenyl)-3- piperidyl 2994 CH CH CH N N1-(3-trifuoromethylphenyl)-3- piperidyl 2995 CH CH CH N N1-(4-trifuoromethylphenyl)-3- piperidyl 2996 CH CH CH N N1-(3,5-difluorophenyl)-3- piperidyl 2997 CH CH CH N N1-(2-difluoromethoxyphenyl)-3- piperidyl 2998 CH CH CH N N1-(3-difluoromethoxyphenyl)-3- piperidyl 2999 CH CH CH N N1-(4-difluoromethoxyphenyl)-3- piperidiyl 3000 CH CH CH N N1-(2-pyridyl)-3-piperidyl 3001 CH CH CH N N 1-(3-pyridyl)-3-piperidyl3002 CH CH CH N N 1-(4-pyridyl)-3-piperidyl 3003 CH CH CH N N1-phenyl-4-piperidyl 3004 CH CH CH N N 1-(2-fluorophenyl)-4-piperidyl3005 CH CH CH N N 1-(3-fluorophenyl)-4-piperidyl 3006 CH CH CH N N1-(4-fluorophenyl)-4-piperidyl 3007 CH CH CH N N1-(2-chlorophenyl)-4-piperidyl 3008 CH CH CH N N1-(3-chlorophenyl)-4-piperidyl 3009 CH CH CH N N1-(4-chlorophenyl)-4-piperidyl 3010 CH CH CH N N1-(2-methylphenyl)-4-piperidyl 3011 CH CH CH N N1-(3-methylphenyl)-4-piperidyl 3012 CH CH CH N N1-(4-methylphenyl)-4-piperidyl 3013 CH CH CH N N1-(2-methoxyphenyl)-4-piperidyl 3014 CH CH CH N N1-(3-methoxyphenyl)-4-piperidyl 3015 CH CH CH N N1-(4-methoxyphenyl)-4-piperidyl 3016 CH CH CH N N1-(2-trifluoromethylphenyl)-4- piperidyl 3017 CH CH CH N N1-(3-trifluoromethylphenyl)-4- piperidyl 3018 CH CH CH N N1-(4-trifluoromethylphenyl)-4- piperidyl 3019 CH CH CH N N1-(3,5-difluorophenyl)-4- piperidyl 3020 CH CH CH N N1-(2-difluoromethoxyphenyl)-4- piperidyl 3021 CH CH CH N N1-(3-difluoromethoxyphenyl)-4- piperidyl 3022 CH CH CH N N1-(4-difluoromethoxyphenyl)-4- piperidyl 3023 CH CH CH N N1-(2-pyridyl)-4-piperidyl 3024 CH CH CH N N 1-(3-pyridyl)-4-piperidyl3025 CH CH CH N N 1-(4-pyridyl)-4-piperidyl 3026 CH CH CH N N3-hydroxymethyl-1-phenyl-4- piperidyl 3027 CH CH CH N N3-methoxycarbonyl-1-phenyl-4- piperidyl 3028 CH CH CH N N3-ethoxycarbonyl-1-phenyl-4- piperidyl 3029 CH CH CH N N3-isopropoxycarbonyl-1-phenyl-4- piperidyl 3030 CH CH CH N N4-phenylcyclohexyl 3031 CH CH CH N N 4-(2-fluorophenyl)cyclohexyl 3032CH CH CH N N 4-(3-fluorophenyl)cyclohexyl 3033 CH CH CH N N4-(4-fluorophenyl)cyclohexyl 3034 CH CH CH N N4-(2-chlorophenyl)cyclohexyl 3035 CH CH CH N N4-(3-chlorophenyl)cyclohexyl 3036 CH CH CH N N4-(4-chlorophenyl)cyclohexyl 3037 CH CH CH N N4-(2-methylphenyl)cyclohexyl 3038 CH CH CH N N4-(3-methylphenyl)cyclohexyl 3039 CH CH CH N N4-(4-methylphenyl)cyclohexyl 3040 CH CH CH N N4-(2-methoxyphenyl)cyclohexyl 3041 CH CH CH N N4-(3-methoxyphenyl)cyclohexyl 3042 CH CH CH N N4-(4-methoxyphenyl)cyclohexyl 3043 CH CH CH N N4-(2-trifluoromethylphenyl)cyclo- hexyl 3044 CH CH CH N N4-(3-trifluoromethylphenyl)cyclo- hexyl 3045 CH CH CH N N4-(4-trifluoromethylphenyl)cyclo- hexyl 3046 CH CH CH N N4-(3,5-difluorophenyl)cyclohexyl 3047 CH CH CH N N4-(3-acetylphenyl)cyclohexyl 3048 CH CH CH N N4-(3-cyanophenyl)cyclohexyl 3049 CH CH CH N N4-(2-difluoromethoxyphenyl)cyclo- hexyl 3050 CH CH CH N N4-(3-difluoromethoxyphenyl)cyclo- hexyl 3051 CH CH CH N N4-(4-difluoromethoxyphenyl)cyclo- hexyl 3052 CH CH CH N N4-(2-pyridyl)cyclohexyl 3053 CH CH CH N N 4-(3-pyridyl)cyclohexyl 3054CH CH CH N N 4-(4-pyridyl)cyclohexyl 3055 CH CH CH N N4-(4-fluoro-3-pyridyl)cyclohexyl 3056 CH CH CH N N4-(3-quinolyl)cyclohexyl 3057 CH CH CH N N 4-(3-fluorophenyl)-4-hydroxy-cyclohexyl 3058 CH CH CH N N 3-phenylcyclohexyl 3059 CH CH CH N N3-phenylcyclopentyl 3060 CH CH CH N N 6-phenyl-3-tetrahydropyranyl 3061CH CH CH N N 6-(3-fluorophenyl)-3-tetrahydro- pyranyl 3062 CH CH CH N N2-phenylcyclopropyl 3063 CH CH CH N N 2-(2-pyridyl)cyclopropyl 3064 CHCH CH N N 2-(3-pyridyl)cyclopropyl 3065 CH CH CH N N2-(4-pyridyl)cyclopropyl 3066 CH CH CH N N 2-(3-fluorophenyl)cyclopropyl3067 CH CH CH N N 2-indanyl 3068 CH CH CH N N 2-tetrahydronaphthyl 3069CH CH CH N N 6-methoxy-2-tetrahydronaphthyl 3070 CH CH CH N N benzyl3071 CH CH CH N N phenethyl 3072 CH CH CH N N 3-phenylpropyl 3073 CH CHCH N N 4-phenylbutyl 3074 CH CH CH N N 2-methoxyphenethyl 3075 CH CH CHN N 3-methoxyphenethyl 3076 CH CH CH N N 4-methoxyphenethyl 3077 CH CHCH N N 4-fluorophenethyl 3078 CH CH CH N N 4-bromophenethyl 3079 CH CHCH N N 4-chlorophenethyl 3080 CH CH CH N N 3-trifluoromethylphenethyl3081 CH CH CH N N 3,4-dimethoxyphenethyl 3082 CH CH CH N N3-propoxyphenethyl 3083 CH CH CH N N 3,5-difluorophenethyl 3084 CH CH CHN N 4-dimethylaminophenethyl 3085 CH CH CH N N3-difluoromethoxyphenethyl 3086 CH CH CH N N 2-methylphenethyl 3087 CHCH CH N N 4-acetylphenethyl 3088 CH CH CH N N4-dimethylamino-2-methoxyphenethyl 3089 CH CH CH N N cyclohexylethyl3090 CH CH CH N N 2-(2-pyridyl)ethyl 3091 CH CH CH N N2-(3-pyridyl)ethyl 3092 CH CH CH N N 2-(4-pyridyl)ethyl 3093 CH CH CH NN 2-(2-quinolyl)ethyl 3094 CH CH CH N N 2-(3-quinolyl)ethyl 3095 CH CHCH N N 2-(4-quinolyl)ethyl 3096 CH CH CH N N 2-(6-quinolyl)ethyl 3097 CHCH CH N N 2-(2-indolyl)ethyl 3098 CH CH CH N N 2-(3-indolyl)ethyl 3099CH CH CH N N 2-(7-aza-3-indolyl)ethyl 3100 CH CH CH N N2-(benzimidazolyl)ethyl 3101 CH CH CH N N 2-(benzoxazolyl)ethyl 3102 CHCH CH N N 2-(benzothiazolyl)ethyl 3103 CH CH CH N N 2-(1-naphthyl)ethyl3104 CH CH CH N N 2-(2-naphthyl)ethyl 3105 CH CH CH N N1-(hydroxymethyl)-2-phenylethyl 3106 CH CH CH N N1-(methoxycarbonyl)-2-phenylethyl 3107 CH CH CH N N1-(ethoxycarbonyl)-2-phenylethyl 3108 CH CH CH N N1-carboxy-2-phenylethyl 3109 CH CH CH N N1-(benzyloxycarbonyl)-2-phenyl- ethyl 3110 CH CH CH N N1-(phenoxymethyl)-2-phenylethyl 3111 CH CH CH N N1-(benzyloxymethyl)-2-phenylethyl 3112 CH CH CH N N1-(benzylcarbamoyl)-2-phenylethyl 3113 CH CH CH N N1-(N-methylbenzylcarbamoyl)-2- phenylethyl 3114 CH CH CH N N1-(phenylcarbamoyl)-2-phenylethyl 3115 CH CH CH N N1-(N-methylphenylcarbamoyl)-2- phenylethyl 3116 CH CH CH N N1-(N-benzylaminomethyl)-2- phenylethyl 3117 CH CH CH N N1-(N-benzyl-N-methylaminomethyl)- 2-phenylethyl 3118 CH CH CH N N1-(anilinomethyl)-2-phenylethyl 3119 CH CH CH N N1-(N-methylanilinomethyl)-2- phenylethyl 3120 CH CH CH N N1-(N-methylaminomethyl)-2- phenylethyl 3121 CH CH CH N N1-(N-ethylaminomethyl)-2- phenylethyl 3122 CH CH CH N N1-(N-isobutylaminomethyl)-2- phenylethyl 3123 CH CH CH N N1-(N-cyclopropylmethylamino- methyl)-2-phenylethyl 3124 CH CH CH N N1-(aminomethyl)-2-phenylethyl 3125 CH CH CH N N1-benzyl-2-(2-pyridylmethyl- amino)ethyl 3126 CH CH CH N N1-benzyl-2-(3-pyridylmethyl- amino)ethyl 3127 CH CH CH N N1-benzyl-2-(4-pyridylmethyl- amino)ethyl 3128 CH CH CH N N2-phenyl-1-(2-pyridylmethyl- carbamoyl)ethyl 3129 CH CH CH N N2-phenyl-1-(3-pyridylmethyl- carbamoyl)ethyl 3130 CH CH CH N N2-phenyl-1-(4-pyridylmethyl- carbamoyl)ethyl 3131 CH CH CH N N2-hydroxy-2-phenylethyl 3132 CH CH CH N N benzoylmethyl 3133 CH CH CH NN 1-(benzyloxycarbonyl)-2-(3- indolyl)ethyl 3134 CH CH CH N N1-(benzyloxycarbonyl)-2- cyclohexylethyl 3135 CH CH CH N N1-(phenoxymethyl)-2-(3- indolyl)ethyl 3136 CH CH CH N N2-(2-methoxyphenoxy)ethyl 3137 CH CH CH N N 1-(benzylcarbamoyl)-2-cyclohexylethyl 3138 CH CH CH N N 1-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 3139 CH CH CH N N 1-(phenylcarbamoyl)-2- cyclohexylethyl3140 CH CH CH N N 1-(N-methylphenylcarbamoyl)-2- cyclohexylethyl 3141 CHCH CH N N 1-(benzyloxycarbonyl)-2-(3- pyridyl)ethyl 3142 CH CH CH N N1-(benzylaminomethyl)-2-(3- pyridyl)ethyl 3143 CH CH CH N N1-(benzylcarbamoyl)-2-(4- pyridyl)ethyl 3144 CH CH CH N N1-(4-pyridylmethylcarbamoyl)-2-(4- fluorophenyl)ethyl 3145 CH CH CH N N1-(benzylcarbamoyl)-2-(7-aza-3- indolyl)ethyl 3146 CH CH CH N N1-(benzyloxymethyl)-2-(2- indolyl)ethyl 3147 CH CH CH N N1-(N-benzyl-N-methylaminomethyl)- 2-(3-pyridyl)ethyl 3148 CH CH CH N N1-(N-methylbenzylcarbamoyl)-2-(3- pyridyl)ethyl 3149 CH CH CH N N2-hydroxy-2-(4-dimethylamino- phenyl)ethyl 3150 CH CH CH N N2-hydroxy-2-(2-quinolyl)ethyl 3151 CH CH CH N N2-hydroxy-2-(3-quinolyl)ethyl 3152 CH CH CH N N2-hydroxy-2-(4-quinolyl)ethyl 3153 CH CH CH N N3-hydroxy-2-(3,5-difluoro- phenyl)ethyl 3154 CH CH CH N N1-carboxy-2-cyclohexylethyl 3155 CH CH CH N N2-hydroxy-2-(6-quinolyl)ethyl 3156 CH CH CH N N2-(benzylamino)-2-phenylethyl 3157 CH CH CH N N2-amino-2-(2-naphthyl)propyl 3158 CH CH CH N N 2-(phenylamino)ethyl 3159CH CH CH N N diphenylmethyl 3160 CH CH CH N N 2,2-diphenylethyl 3161 CHCH CH N N 2-phenyl-2-(2-pyridyl)ethyl 3162 CH CH CH N N2-phenyl-2-(3-pyridyl)ethyl 3163 CH CH CH N N2-phenyl-2-(4-pyridyl)ethyl 3164 CH CH CH N N 2-phenoxy-2-phenylethyl3165 CH CH CH N N 2-(benzyloxy)-2-phenylethyl

TABLE 4

No. A—Ar¹—R⁰ 3157′ 1-phenyl-3-pyrrolidinyl 3158′1-(2-fluorophenyl)-3-pyrrolidinyl 3159′1-(3-fluorophenyl)-3-pyrrolidinyl 3160′1-(4-fluorophenyl)-3-pyrrolidinyl 3161′1-(2-chlorophenyl)-3-pyrrolidinyl 3162′1-(3-chlorophenyl)-3-pyrrolidinyl 3163′1-(4-chlorophenyl)-3-pyrrolidinyl 3164′1-(2-methylphenyl)-3-pyrrolidinyl 3165′1-(3-methyiphenyl)-3-pyrrolidinyl 3166 1-(4-methylphenyl)-3-pyrrolidinyl3167 1-(2-methoxyphenyl)-3-pyrrolidinyl 31681-(3-methoxyphenyl)-3-pyrrolidinyl 31691-(4-methoxyphenyl)-3-pyrrolidinyl 31701-(2-trifluoromethylphenyl)-3-pyrrolidinyl 31711-(3-trifluoromethylphenyl)-3-pyrrolidinyl 31721-(4-trifluoromethylphenyl)-3-pyrrolidinyl 31731-(3,5-difluorophenyl)-3-pyrrolidinyl 31741-(2-difluoromethoxyphenyl)-3-pyrrolidinyl 31751-(3-difluoromethoxyphenyl)-3-pyrrolidinyl 31761-(4-difluoromethoxyphenyl)-3-pyrrolidinyl 31771-(2-pyridyl)-3-pyrrolidinyl 3178 1-(3-pyridyl)-3-pyrrolidinyl 31791-(4-pyridyl)-3-pyrrolidinyl 3180 1-(2-pyrimidinyl)-3-pyrrolidinyl 31815-oxo-1-phenyl-3-pyrrolidinyl 3182 1-phenyl-3-piperidyl 31831-(2-fluorophenyl)-3-piperidyl 3184 1-(3-fluorophenyl)-3-piperidyl 31851-(4-fluorophenyl)-3-piperidyl 3186 1-(2-chlorophenyl)-3-piperidyl 31871-(3-chlorophenyl)-3-piperidyl 3188 1-(4-chlorophenyl)-3-piperidyl 31891-(2-methylphenyl)-3-piperidyl 3190 1-(3-methylphenyl)-3-piperidyl 31911-(4-methylphenyl)-3-piperidyl 3192 1-(2-methoxyphenyl)-3-piperidyl 31931-(3-methoxyphenyl)-3-piperidyl 3194 1-(4-methoxyphenyl)-3-piperidyl3195 1-(2-trifluoromethylphenyl)-3-piperidyl 31961-(3-trifluoromethylphenyl)-3-piperidyl 31971-(4-trifluoromethylphenyl)-3-piperidyl 31981-(3,5-difluorophenyl)-3-piperidyl 31991-(2-difluoromethoxyphenyl)-3-piperidyl 32001-(3-difluoromethoxyphenyl)-3-piperidyl 32011-(4-difluoromethoxyphenyl)-3-piperidyl 3202 1-(2-pyridyl)-3-piperidyl3203 1-(3-pyridyl)-3-piperidyl 3204 1-(4-pyridyl)-3-piperidyl 32051-phenyl-4-piperidyl 3206 1-(2-fluorophenyl)-4-piperidyl 32071-(3-fluorophenyl)-4-piperidyl 3208 1-(4-fluorophenyl)-4-piperidyl 32091-(2-chlorophenyl)-4-piperidyl 3210 1-(3-chlorophenyl)-4-piperidyl 32111-(4-chlorophenyl)-4-piperidyl 3212 1-(2-methylphenyl)-4-piperidyl 32131-(3-methylphenyl)-4-piperidyl 3214 1-(4-methylphenyl)-4-piperidyl 32151-(2-methoxyphenyl)-4-piperidyl 3216 1-(3-methoxyphenyl)-4-piperidyl3217 1-(4-methoxyphenyl)-4-piperidyl 32181-(2-trifluoromethylphenyl)-4-piperidyl 32191-(3-trifluoromethylphenyl)-4-piperidyl 32201-(4-trifluoromethylphenyl)-4-piperidyl 32211-(3,5-difluorophenyl)-4-piperidyl 32221-(2-difluoromethoxyphenyl)-4-piperidyl 32231-(3-difluoromethoxyphenyl)-4-piperidyl 32241-(4-difluoromethoxyphenyl)-4-piperidyl 3225 1-(2-pyridyl)-4-piperidyl3226 1-(3-pyridyl)-4-piperidyl 3227 1-(4-pyridyl)-4-piperidyl 32283-hydroxymethyl-1-phenyl-4-piperidyl 32293-methoxycarbonyl-1-phenyl-4-piperidyl 32303-ethoxycarbonyl-1-phenyl-4-piperidyl 32313-isopropoxycarbonyl-1-phenyl-4-piperidyl 3232 4-phenylcyclohexyl 32334-(2-fluorophenyl)cyclohexyl 3234 4-(3-fluorophenyl)cyclohexyl 32354-(4-fluorophenyl)cyclohexyl 3236 4-(2-chlorophenyl)cyclohexyl 32374-(3-chlorophenyl)cyclohexyl 3238 4-(4-chlorophenyl)cyclohexyl 32394-(2-methylphenyl)cyclohexyl 3240 4-(3-methylphenyl)cyclohexyl 32414-(4-methylphenyl)cyclohexyl 3242 4-(2-methoxyphenyl)cyclohexyl 32434-(3-methoxyphenyl)cyclohexyl 3244 4-(4-methoxyphenyl)cyclohexyl 32454-(2-trifluoromethylphenyl)cyclohexyl 32464-(3-trifluoromethylphenyl)cyclohexyl 32474-(4-trifluoromethylphenyl)cyclohexyl 32484-(3,5-difluorophenyl)cyclohexyl 3249 4-(3-acetylphenyl)cyclohexyl 32504-(3-cyanophenyl)cyclohexyl 3251 4-(2-difluoromethoxyphenyl)cyclohexyl3252 4-(3-difluoromethoxyphenyl)cyclohexyl 32534-(4-difluoromethoxyphenyl)cyclohexyl 3254 4-(2-pyridyl)cyclohexyl 32554-(3-pyridyl)cyclohexyl 3256 4-(4-pyridyl)cyclohexyl 32574-(4-fluoro-3-pyridyl)cyclohexyl 3258 4-(3-quinolyl)cyclohexyl 32594-(3-fluorophenyl)-4-hydroxycyclohexyl 3260 3-phenylcyclohexyl 32613-phenylcyclopentyl 3262 6-phenyl-3-tetrahydropyranyl 32636-(3-fluorophenyl)-3-tetrahydropyranyl 3264 2-phenylcyclopropyl 32652-(2-pyridyl)cyclopropyl 3266 2-(3-pyridyl)cyclopropyl 32672-(4-pyridyl)cyclopropyl 3268 2-(3-fluorophenyl)cyclopropyl 32692-indanyl 3270 2-tetrahydronaphthyl 3271 6-methoxy-2-tetrahydronaphthyl3272 benzyl 3273 phenethyl 3274 3-phenylpropyl 3275 4-phenylbutyl 32762-methoxyphenethyl 3277 3-methoxyphenethyl 3278 4-methoxyphenethyl 32794-fluorophenethyl 3280 4-bromophenethyl 3281 4-chlorophenethyl 32823-trifluoromethylphenethyl 3283 3,4-dimethoxyphenethyl 32843-propoxyphenethyl 3285 3,5-difluorophenethyl 32864-dimethylaminophenethyl 3287 3-difluoromethoxyphenethyl 32882-methylphenethyl 3289 4-acetylphenethyl 32904-dimethylamino-2-methoxyphenethyl 3291 cyclohexylethyl 32922-(2-pyridyl)ethyl 3293 2-(3-pyridyl)ethyl 3294 2-(4-pyridyl)ethyl 32952-(2-quinolyl)ethyl 3296 2-(3-quinolyl)ethyl 3297 2-(4-quinolyl)ethyl3298 2-(6-quinolyl)ethyl 3299 2-(2-indolyl)ethyl 3300 2-(3-indolyl)ethyl3301 2-(7-aza-3-indolyl)ethyl 3302 2-(benzimidazolyl)ethyl 33032-(benzoxazolyl)ethyl 3304 2-(benzothiazolyl)ethyl 33052-(1-naphthyl)ethyl 3306 2-(2-naphthyl)ethyl 33071-(hydroxymethyl)-2-phenylethyl 3308 1-(methoxycarbonyl)-2-phenylethyl3309 1-(ethoxycarbonyl)-2-phenylethyl 3310 1-carboxy-2-phenylethyl 33111-(benzyloxycarbonyl)-2-phenylethyl 3312 1-(phenoxymethyl)-2-phenylethyl3313 1-(benzyloxymethyl)-2-phenylethyl 33141-(benzylcarbamoyl)-2-phenylethyl 33151-(N-methylbenzylcarbamoyl)-2-phenylethyl 33161-(phenylcarbamoyl)-2-phenylethyl 33171-(N-methylphenylcarbamoyl)-2-phenylethyl 33181-(N-benzylaminomethyl)-2-phenylethyl 33191-(N-benzyl-N-methylaminomethyl)-2-phenylethyl 33201-(anilinomethyl)-2-phenylethyl 33211-(N-methylanilinomethyl)-2-phenylethyl 33221-(N-methylaminomethyl)-2-phenylethyl 33231-(N-ethylaminomethyl)-2-phenylethyl 33241-(N-isobutylaminomethyl)-2-phenylethyl 33251-(N-cyclopropylmethylaminomethyl)-2-phenylethyl 33261-(aminomethyl)-2-phenylethyl 33271-benzyl-2-(2-pyridylmethylamino)ethyl 33281-benzyl-2-(3-pyridylmethylamino)ethyl 33291-benzyl-2-(4-pyridylmethylaniino)ethyl 33302-phenyl-1-(2-pyridylmethylcarbamoyl)ethyl 33312-phenyl-1-(3-pyridylmethylcarbamoyl)ethyl 33322-phenyl-1-(4-pyridylmethylcarbamoyl)ethyl 3333 2-hydroxy-2-phenylethyl3334 benzoylmethyl 3335 1-(benzyloxycarbonyl)-2-(3-indolyl)ethyl 33361-(benzyloxycarbonyl)-2-cyclohexylethyl 33371-(phenoxymethyl)-2-(3-indolyl)ethyl 3338 2-(2-methoxyphenoxyy)ethyl3339 1-(benzylcarbamoyl)-2-cyclohexylethyl 33401-(N-methylbenzylcarbamoyl)-2-cyclohexylethyl 33411-(phenylcarbamoyl)-2-cyclohexylethyl 33421-(N-methylphenylcarbamoyl)-2-cyclohexylethyl 33431-(benzyloxycarbonyl)-2-(3-pyridyl)ethyl 33441-(benzylaminomethyl)-2-(3-pyridyl)ethyl 33451-(benzylcarbamoyl)-2-(4-pyridyl)ethyl 33461-(4-pyridylmethylcarbamoyl)-2-(4-fluorophenyl)ethyl 33471-(benzylcarbamoyl)-2-(7-aza-3-indolyl)ethyl 33481-(benzyloxymethyl)-2-(2-indolyl)ethyl 33491-(N-benzyl-N-methylaminomethyl)-2-(3-pyridyl)ethyl 33501-(N-methylbenzylcarbamoyl)-2-(3-pyridyl)ethyl 33512-hydroxy-2-(4-dimethylaminophenyl)ethyl 33522-hydroxy-2-(2-quinolyl)ethyl 3353 2-hydroxy-2-(3-quinolyl)ethyl 33542-hydroxy-2-(4-quinolyl)ethyl 3355 2-hydroxy-2-(3,5-difluorophenyl)ethyl3356 1-carboxy-2-cyclohexylethyl 3357 2-hydroxy-2-(6-quinolyl)ethyl 33582-(benzylamino)-2-phenylethyl 3359 2-amino-2-(2-naphthyl)propyl 33602-(phenylamino)ethyl 3361 diphenylmethyl 3362 2,2-diphenylethyl 33632-phenyl-2-(2-pyridyl)ethyl 3364 2-phenyl-2-(3-pyridyl)ethyl 33652-phenyl-2-(4-pyridyl)ethyl 3366 2-phenoxy-2-phenylethyl 33672-(benzyloxy)-2-phenylethyl

Among the above compounds, the preferred examples are

-   trans-3′-oxo-N-(trans-4-phenylcyclohexyl)spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[(3S)-1-(4-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[1-(4-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-3′-oxo-N-(1,2,3,4-tetrahydro-2-naphthyl)spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-(6-methoxy-1,2,3,4-tetrahydro-2-naphthyl)-3-oxo-spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3′-oxo-N-[(3S)-5-oxo-1-phenyl-3-pyrrolidinyl]spiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3-oxo-N-[(3S)-1-(3-trifluoromethylphenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3-oxo-N-[(3S)-1-(2-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3-oxo-N-[(3S)-1-(3-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[trans-4-(4-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[(3S)-1-(3,5-difluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[3-(3-fluorophenyl)-tetrahydropyran-6-yl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[trans-4-(2-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-benzhydryl-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[1-(3-fluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-[1-(2-pyridyl)-4-piperidyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-(1-phenyl-3-piperidyl)spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[1-(3,5-difluorophenyl)-3-piperidyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-[1-(2-pyridyl)-3-piperidyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-[(3S)-1-phenyl-3-pyrrolidinyl]-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-[(3R)-1-phenyl-3-pyrrolidinyl]-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-(2-phenylcyclopropyl)spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-[2-(3-pyridyl)cyclopropyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[1-benzylcarbamoyl-2-(4-pyridyl)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[2-(4-fluorophenyl)-1-[(4-pyridylmethyl)carbamoyl]-ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-(2-hydroxy-2-phenylethyl)-1-methanesulfonylspiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-(benzoylmethyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-benzyl-2-(N-benzylmethylamino)ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-phenylethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-(3-pyridyl)-ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-(4-dimethylaminophenethyl)-1-methanesulfonylspiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-[2-(3-quinolyl)ethyl]spiro-[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[2-(4-dimethylaminophenyl)-2-hydroxyethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[2-hydroxy-2-(3-quinolyl)ethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[2-(3,5-difluorophenyl)-2-hydroxyethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-benzyl-2-[(3-pyridylmethyl)amino]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-benzyl-2-[(2-pyridylmethyl)amino]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-2-anilino-1-benzylethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-[(S)-1-benzyl-2-(isobutylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-1-methanesulfonyl-N-[2-phenyl-1-(methoxycarbonyl)-ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   trans-N-(1-hydroxymethyl-2-phenylethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide,-   1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide,-   3-oxo-N-(1-phenyl-3-piperidyl)spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide,-   3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide,-   N-[1-benzylcarbamoyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   N-[(S)-1-benzyloxymethyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   N-[(S)-1-benzylcarbamoyl-2-phenylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide,-   1-methanesulfonyl-N-phenethylspiro[indoline-3,4′-piperidine]-1′-carboxamide,-   1-methanesulfonyl-N-(3-phenylpropyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide,-   1-methanesulfonyl-N-(4-phenylbutyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide,-   N-(4-bromophenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide,-   N-(3,4-dimethoxyphenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide,-   1-methanesulfonyl-N-(3-methoxyphenethyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide,-   N-(4-dimethylamino-2-methoxyphenethyl)-1-methanesulfonyl-spiro[indoline-3,4′-piperidine]-1′-carboxamide,-   N-[(S)-1-benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   N-[(R)-1-benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   N-[(S)-1-benzyloxycarbonyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   3,4-dihydro-N-(3-methoxyphenethyl)-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide,-   trans-N-[1-(3-trifluoromethylphenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3′-oxo-N-[5-oxo-1-(2-fluorophenyl)-3-pyrrolidinyl]-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-3′-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-3-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-N-[trans-4-(3-trifluoromethylphenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,-   trans-3′-oxo-N-[2-oxo-1-phenyl-4-piperidyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-3′-oxo-N-[2-oxo-1-(3-fluorophenyl)-4-piperidyl]spiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[trans-2-(2-fluorophenyl)cyclopropyl]-3′-oxospiro-[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,-   trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide    or-   trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,    and the like.

The processes for producing the compounds of the present invention areillustrated below.

The compounds (I) of the present invention can be prepared, for example,by the following production processes or the methods shown in Examples,but Manufacturing methods of the compounds (I) of the present inventionare not limited to these embodiments.

Production Process 1

A compound of the formula (II):

(wherein

A^(p) is a straight-chain hydrocarbon having 1 to 6 carbon atoms, whichis optionally substituted by a substituent selected from the groupconsisting of di-lower alkylamino, lower alkoxy, lower alkoxycarbonyl,lower alkylene, aryl, heteroaryl, —R^(ap), optionally protected oxo,optionally protected amino, optionally protected lower alkylamino andoptionally protected hydroxy, and is optionally intervened by oxygen ornitrogen atom;

Ar^(1p) is aryl or heteroaryl, any of which is optionally substituted bya substituent selected from the group consisting of halogen, nitro,lower alkyl, halo-lower alkyl, cyclo-lower alkyl, lower alkenyl, loweralkoxy, halo-lower alkoxy, di-lower alkylamino, lower alkylthio, loweralkanoyl, lower alkoxycarbonyl, -Q^(p)-Ar^(2p), optionally protectedoxo, optionally protected hydroxy-lower alkyl, optionally protectedlower alkylamino and optionally protected carboxyl;

Ar^(2p) is aryl or heteroaryl, any of which is optionally substituted bya substituent selected from the group consisting of halogen, cyano,lower alkyl, halo-lower alkyl, lower alkoxy, halo-lower alkoxy, di-loweralkylamino, lower alkanoyl, aryl, optionally protected hydroxy-loweralkyl, optionally protected hydroxy and optionally protected loweralkylamino;

Ar³ is phenyl which is optionally substituted by halogen or nitro;

Q^(p) is a single bond or optionally protected carbonyl;

R^(ap) is lower alkyl which is optionally substituted by a substituentselected from the group consisting of di-lower alkylamino, optionallyprotected amino, optionally protected lower alkylamino, optionallyprotected hydroxy, and cyclo-lower alkyl, aryl and heteroaryl, the lastthree groups being optionally substituted by fluorine;

R^(0p) is hydrogen, or lower alkylene attached to an arbitrary, bondableposition of A^(P)) is reacted with a compound of the formula (III):

(wherein t, u, v and w are independently methine or nitrogen atom, saidmethine being optionally substituted by a substituent selected from thegroup consisting of halogen, lower alkyl, lower alkoxy and optionallyprotected hydroxy, and at least two of t, u, v and w are said methinegroup; n, X and Y have the same meaning as defined above), to provide acompound of the formula (IV-1):

(wherein A^(p), Ar^(1p), n, R^(0p), t, u, v, w, X and Y have the samemeaning as defined above), optionally followed by removal of theprotecting group(s) from the compound (IV-1), thereby a compound of theformula (I-1):

(wherein A, Ar¹, n, R⁰, T, U, V, W, X and Y have the same meaning asdefined above) can be prepared.

The present process is a process for preparing a compound of the formula(I) wherein Z is nitrogen atom, that is, a compound of the formula(I-1).

In the above reaction, when a reactant has an amino, hydroxy, carboxyl,oxo, carbonyl or the like which does not participate in the reaction,the reaction may be carried out after protecting said amino, hydroxy,carboxyl, oxo or carbonyl with an amino-protecting group, ahydroxy-protecting group, a carboxyl-protecting group, or an oxo- orcarbonyl-protecting group, and said protecting groups may be removedafter completion of the reaction.

The “amino-protecting group” includes, for example, aralkyl (e.g.benzyl, p-methoxybenzyl, 3,4-dimethoxybenzyl, o-nitrobenzyl,p-nitrobenzyl, benzhydryl, trityl); lower alkanoyl (e.g. formyl, acetyl,propionyl, butyryl, pivaloyl); benzoyl; arylalkanoyl (e.g. phenylacetyl,phenoxyacetyl); lower alkoxycarbonyl (e.g. methoxycarbonyl,ethoxycarbonyl, propyloxycarbonyl, tert-butoxycarbonyl);aralkyloxycarbonyl (e.g. benzyloxycarbonyl, p-nitrobenzyloxycarbonyl,phenethyloxycarbonyl); lower alkylsilyl (e.g. trimethylsilyl,tert-butyldimethylsilyl); among which the preferred examples are acetyl,pivaloyl, benzoyl, ethoxycarbonyl, tert-butoxycarbonyl, and the like.

The “hydroxy-protecting group” includes, for example, lower alkyl (e.g.methyl, ethyl, propyl, isopropyl, tert-butyl); lower alkylsilyl (e.g.trimethylsilyl, tert-butyldimethylsilyl); lower alkoxymethyl (e.g.methoxymethyl, 2-methoxyethoxymethyl); tetrahydropyranyl;trimethylsilylethoxymethyl; aralkyl (e.g. benzyl, p-methoxybenzyl,2,3-dimethoxybenzyl, o-nitrobenzyl, p-nitrobenzyl, trityl); acyl (e.g.formyl, acetyl); among which the preferred examples are methyl,methoxymethyl, tetrahydropyranyl, trityl, trimethylsilylethoxymethyl,tert-butyldimethylsilyl, acetyl, and the like.

The “carboxyl-protecting group” includes, for example, lower alkyl (e.g.methyl, ethyl, propyl, isopropyl, tert-butyl); halo-lower alkyl (e.g.2,2,2-trichloroethyl); lower alkenyl (e.g. 2-propenyl); aralkyl (e.g.benzyl, p-methoxybenzyl, p-nitrobenzyl, benzhydryl, trityl), among whichthe preferred examples are methyl, ethyl, tert-butyl, 2-propenyl,benzyl, p-methoxybenzyl, benzhydryl, and the like.

The “oxo- or carbonyl-protecting group” includes, for example, acetal(e.g. ethylene ketal, trimethylene ketal, dimethyl ketal), ketal, andthe like.

The reaction between a compound of the formula (II) and a compound ofthe formula (III) is usually carried out by employing equivalent toexcess moles, preferably equivalent to 1.5 moles of the compound of theformula (III) based on 1 mole of the compound (II).

The reaction is usually carried out in an inert solvent, and preferableexamples of such inert solvent are methylene chloride, chloroform,tetrahydrofuran, dimethylformamide, dimethylsulfoxide, etc., or amixture thereof and the like.

It is preferable to carry out the above reaction in the presence of abase, and examples of such base are organic bases (e.g. triethylamine,diisopropylethylamine, pyridine, 4-dimethylaminopyridine) or inorganicbases (e.g. sodium hydroxide, potassium hydroxide).

The amount of the said base employed is usually equivalent to excessmoles, preferably 1 to 5 moles based on 1 mole of a compound of theformula (II).

The reaction temperature is usually from −30° C. to 200° C., preferablyfrom 20° C. to 100° C.

The reaction time is usually from 5 minutes to 7 days, preferably from30 minutes to 24 hours.

Usual workup procedures are applied after completion of the reaction toobtain a crude product of a compound of the formula (IV-1). Theresulting compound of the formula (IV-1) is, with or withoutpurification according to the common method, subjected to, if desired,proper combination of removal of the protecting group(s) for amino,hydroxy, carboxyl, oxo and carbonyl, thereby a compound of the formula(I-1) can be prepared.

Although the method for the removal of said protecting groups dependsupon the kinds of the protecting groups, the stability of a desiredcompound (I-1), etc., it is carried out by, for example, a solvolysisusing an acid or a base, that is, for example a method wherein 0.01 moleto a large excess of an acid, preferably trifluoroacetic acid, formicacid, hydrochloric acid and the like, or equivalent moles to a largeexcess of base, preferably potassium hydroxide, calcium hydroxide andthe like is acted; a chemical reduction using a metal hydride complex;or a catalytic reduction using a palladium-carbon catalyst, aRaney-nickel catalyst, etc., according to, for example, a methoddescribed in the literature (Protective Groups in Organic Synthesis, T.W. Greene, John Wiley & Sons, (1981)) or its similar methods.

Production Process 2

A compound of the formula (V):

(wherein A^(p), Ar^(1p) and R^(0p) have the same meaning as definedabove) is reacted with a carboxylic acid of the formula (VI):

(wherein n, t, u, v, w, X and Y have the same meaning as defined above)or a reactive derivative thereof to provide a compound of the formula(IV-2):

(wherein A^(p), Ar^(1p), n, R^(0p), t, u, v, w, X and Y have the samemeaning as defined above), optionally followed by removal of theprotecting group (s) from the compound (IV-2), thereby a compound of theformula (I-2):

(wherein A, Ar¹, n, R⁰, T, U, V, W, X and Y have the same meaning asdefined above) can be prepared.

The present process is a process for preparing a compound of the formula(I) wherein Z is methine group, that is, a compound of the formula(I-2).

The reaction between a compound of the formula (V) and a carboxylic acidof the formula (VI) is usually carried out by employing 0.5 to excessmoles, preferably 1 mole to 1.5 moles of the carboxylic acid of theformula (VI) based on 1 mole of the compound of the formula (V).

The reaction is usually carried out in an inert solvent, and thepreferable examples of such inert solvent are methylene chloride,chloroform, tetrahydrofuran, dimethylformamide, pyridine, etc., or amixture thereof and the like.

It is preferable to carry out the above reaction in the presence of acondensing agent, and examples of such condensing agent are,N,N′-dicyclohexylcarbodiimide, N,N′-diisopropylcarbodiimide,1-(3-dimethylaminopropyl)-3-ethylcarbodiimide,1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride,benzotriazol-1-yloxy-tris-(dimethylamino)phosphonium-hexafluorophosphate,benzotriazol-1-yloxy-tris-pyrrolidinophosphonium-hexafluorophosphate,bromotris-(dimethylamino)phosphonium-hexafluorophosphate,diphenylphosphoryl azide, 1,1′-carbonyldiimidazole, and the like.

The amount of said condensing agent employed may be usually 1 mole toexcess mole, preferably 1 to 1.5 moles based on 1 mole of a compound ofthe formula (VI).

The reaction temperature is usually from −50° C. to 100° C., preferablyfrom −20° C. to 50° C.

The reaction time is usually from 30 minutes to 7 days, preferably from1 hour to 24 hours.

A compound of the formula (I-2) is also produced by reacting a compoundof the formula (V) with an activated derivative of the carboxylic acidof the formula (VI) instead of the carboxylic acid of the formula (VI).

Examples of the activated derivatives of carboxylic acid of the formula(VI) include acid halides, mixed anhydrides, activated esters, activatedamides, and the like.

The acid halides of carboxylic acid of the formula (VI) may be obtainedby reacting a carboxylic acid of the formula (VI) with a halogenatingagent according to the conventional method. The halogenating agentincludes, for example, thionyl chloride, phosphorus trichloride,phosphorus pentachloride, phosphorus oxychloride, phosphorus tribromide,oxalyl chloride, phosgene, and the like.

The mixed anhydrides of carboxylic acid of the formula (VI) may beobtained by reacting a carboxylic acid of the formula (VI) with an alkylchlorocarbonate such as ethyl chlorocarbonate, etc.; an aliphaticcarboxylic acid chloride such as pivaloyl chloride, etc., and the likeaccording to the conventional method.

The activated esters of carboxylic acid of the formula (VI) may beobtained by reacting a carboxylic acid of the formula (VI) with anN-hydroxy compound such as N-hydroxysuccinimide, N-hydroxyphthalimide,1-hydroxybenzotriazole, etc.; a phenol compound such as 4-nitrophenol,2,4-dinitrophenol, 2,4,5-trichlorophenol, pentachlorophenol, etc., andthe like in the presence of a condensing agent such asN,N′-dicyclohexylcarbodiimide,1-(3-dimethylaminopropyl)-3-ethylcarbodiimide, etc. according to theconventional method.

The activated amides of carboxylic acid of the formula (VI) may beobtained by reacting a carboxylic acid of the formula (VI) with, forexample, 1,1′-carbonyldiimidazole, 1,1′-carbonylbis(2-methylimidazole)according to the conventional method.

The reaction between a compound of the formula (V) and an activatedderivative of carboxylic acid of the formula (VI) is usually carried outby employing 0.5 to excess moles, preferably 1 to 1.5 moles of theactivated derivative of carboxylic acid of the formula (VI) based on 1mole of the compound of the formula (V).

The reaction is usually carried out in an inert solvent, and thepreferable examples of such inert solvent are methylene chloride,chloroform, tetrahydrofuran, dimethylformamide, pyridine, etc., or amixture thereof and the like.

Although the above reaction proceeds in the absence of a base, it ispreferred to carry out the reaction in the presence of a base to promotethe reaction smoothly.

Examples of such a base are organic bases (e.g. triethylamine,diisopropylethylamine, pyridine, 4-dimethylaminopyridine) or inorganicbases (e.g. sodium hydroxide, potassium hydroxide, sodium carbonate,potassium carbonate, sodium hydrogen carbonate).

The preferable amount of said base is usually 1 to excess moles based on1 mole of a compound of the formula (V). Also, when the base is aliquid, such base can also be used as a solvent.

The reaction temperature is usually from −50° C. to 100° C., preferablyfrom −20° C. to 50° C.

The reaction time is usually from 5 minutes to 7 days, preferably from30 minutes to 24 hours.

A compound of the formula (I-2) can be produced by working up theresulting product in the usual way after removal of the said protectinggroup(s) when the product has a protecting group after completion of thereaction, or by working up the resulting product directly in the usualway when the protecting group is absent.

The removal of the protecting group(s) and the workup procedure may becarried out according to the method described in the above ProductionProcess 1.

The compound of the formula (I-1) or (I-2) may be readily isolated andpurified by the conventional separation technique, and examples of suchtechnique are solvent extraction, recrystallization, columnchromatography, preparative thin layer chromatography and the like.

These compounds can be converted into the pharmaceutically acceptablesalts or esters by the conventional method, and on the contrary, theconversion of the salts or esters into free compounds can also becarried out according to the conventional method.

Compounds of the formula (II), (III), (V) or (VI) is commerciallyavailable, or can be prepared according to the methods described in theliteratures (Japanese Patent Unexamined Publication No. 94/263737-A,U.S. Pat. No. 3,301,857, J. Org. Chem, 40, p. 1427 (1975), InternationalPatent Publication W095/28389 and the like), or analogous methodsthereto or the methods shown below or in Examples, optionally incombination.

Production Process A

In the above reaction scheme, L is halogen; A^(p), Ar^(1p), Ar³ andR^(0p) have the same meaning as defined above.

The present process is a process for preparing a compound of the formula(II). According to the present process, the compound of the formula (II)can be prepared by reacting a compound of the formula (V) with acompound of the formula 1.

The reaction between the compound of the formula (V) and the compound ofthe formula 1 is usually carried out by employing 0.5 to excess moles,preferably equivalent to 1.5 moles of the compound of the formula 1,based on 1 mole of the compound (V).

The reaction is usually carried out in an inert solvent, and thepreferable examples of such inert solvent are methylene chloride,chloroform, tetrahydrofuran, ethyl ether, benzene, toluene,dimethylformamide, etc., or a mixture thereof and the like.

The above reaction is preferably carried out in the presence of a base,and examples of such base are organic bases (e.g. triethylamine,diisopropylethylamine, pyridine, 4-dimethylaminopyridine) or inorganicbases (e.g. sodium hydroxide, potassium hydroxide, sodium carbonate,potassium carbonate, sodium hydrogen carbonate).

The preferable amount of said base is usually equivalent to excess molesbased on 1 mole of a compound of the formula (V). Also, when the base isa liquid, such base can also be used as a solvent.

The reaction temperature is usually from −78° C. to 100° C., preferablyfrom −20° C. to 50° C.

The reaction time is usually from 5 minutes to 7 days, preferably from30 minutes to 24 hours.

A compound of the formula 1 is commercially available, or can beprepared according to the known methods or the methods in Examples, oranalogous methods thereto, optionally in combination.

The utility of compounds of the present invention as a medicament isproved by showing NPY antagonistic activities in the followingpharmacological test.

Pharmacological Test (NPY Binding Inhibition Test)

A sequence coding for human NPY Y5 receptor (c.f. International patentpublication number W096/16542) was cloned into expression vectorspcDNA3, pRc/RSV (made by Invitrogen Inc.) and pCI-neo (made by PromegaInc.). The expression vectors thus obtained were transfected to hostcells COS-7, CHO and LM(tk-) (American Type Culture Collection) bycationic lipid method (Proceedings of the National Academy of Sciencesof the United States of America, vol. 84: p. 7413(1987)) to give NPY Y5receptor expression cells.

A membrane sample prepared from the cells which expressed NPY Y5receptor was incubated together with a test compound and [¹²⁵I]peptideYY(made by NEN) (20,000 cpm) in an assay buffer (25 mM Tris buffer, pH7.4, containing 10 mM magnesium chloride, 1 mM phenylmethylsulfonylfluoride, 0.1% bacitracin and 0.5% bovine serum albumin) at 25° C. for 2hours, then filtered through a glass filter GF/C and washed with 5 mMTris buffer (pH7.4) containing 0.3% BSA. The radioactivity of the cakeon the glass filter was measured. Non-specific binding was measured inthe presence of 1 μM peptide YY, and 50% Inhibitory Concentration (IC₅₀)of the test compound against specific peptideYY binding was determined(Endocrinology, vol. 131: p. 2090(1992)). The results are shown in Table1.

TABLE 1 NPY receptors binding inhibition compounds IC₅₀ (nM) Example 12.5 Example 5 1.7 Example 27 3.6 Example 32 1.7 Example 36 0.80 Example41 1.2 Example 45 0.69 Example 46 2.0

As shown above, the compounds of this invention potently inhibitedpeptideYY (NPY analogue) binding to NPY Y5 receptors.

The compounds of the formula (I) can be administered orally orparenterally and, by formulating into a suitable administrable form, maybe administered as a therapeutic agent for various diseases related toNPY, for example, cardiovascular disorders such as hypertension,nephropathy, heart disease, vasospasm, arteriosclerosis, etc., centralnervous system disorders such as bulimia, depression, anxiety, seizure,epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythmdisorders, schizophrenia, etc., metabolic diseases such as obesity,diabetes, hormone abnormality, hypercholesterolemia, hyperlipidemia,etc., sexual and reproductive dysfunctions, gastro-intestinal disorderssuch as gastro-intestinal motility disorder, respiratory disorders,inflammatory diseases or glaucoma, and the like, particularly preferablybulimia, obesity, diabetes, and the like. In clinical use, the compoundsof this invention may be administered after being formulated, togetherwith pharmaceutically acceptable additives, into an appropriatepreparation according to the mode of administration. As for suchadditives, those which are usually used in the field of pharmaceuticalformulation, for example, gelatin, lactose, sucrose, titanium oxide,starch, crystalline cellulose, hydroxypropyl methylcellulose,carboxymethylcellulose, corn starch, microcrystalline wax, whitepetrolatum, magnesium methasilicate aluminate, anhydrous calciumphosphate, citric acid, trisodium citrate, hydroxypropyl cellulose,sorbitol, sorbitan fatty acid ester, polysorbate, sucrose fatty acidester, polyoxyethylene, hydrogenated castor oil, polyvinylpyrrolidone,magnesium stearate, light silicic anhydride, talc, vegetable oil, benzylalcohol, gum arabic, propylene glycol, polyalkylene glycol, cyclodextrinor hydroxypropyl cyclodextrin, etc. may be used.

The formulations prepared by mixing the compound of the presentinvention with said additives include, for example, solid preparations(e.g. tablets, capsules, granules, powder, suppositories); or liquidpreparations (e.g. syrups, elixirs, injections). Such preparations maybe formulated according to the techniques well-known in the art ofpharmaceutical formulation. Liquid preparations may be in the form ofpreparations which are dissolved or suspended in water or otherappropriate media when used. In the case of injectable preparations inparticular, they may be dissolved or suspended in physiological salineor glucose solution if necessary, optionally together with a buffer or apreservative.

All the said preparations may contain 1.0 to 100 wt. %, preferably 1.0to 60 wt. % of compounds of the present invention and may also containother therapeutically effective compounds.

The compounds of the present invention can be used in combination withother agents useful for treating metabolic disorders and/or eatingdisorders. The individual component of such combinations can beadministered separately at different times or concurrently in divided orsingle combination forms during the course of therapy. The presentinvention is therefore to be understood as embracing all such regimes ofsimultaneous or divided administration and the term “administration” isto be interpreted accordingly. The scope of combinations of thecompounds of this invention with other agents useful for treatingmetabolic disorders and/or eating disorders includes in principle anycombination of any pharmaceutical composition useful for treatingmetabolic disorders and/or eating disorders.

When compounds of the present invention are used clinically, forexample, a daily dose for an adult is 0.01 to 100 mg/kg, preferably 0.03to 3 mg/kg with simultaneous or divided administration when administeredorally, and 0.001 to 10 mg/kg, preferably 0.001 to 0.1 mg/kg withsimultaneous or divided administration when administered parenterally,though the dose and the frequency of administration may vary dependingupon the sex, age, body weight, degree of symptoms, and type and rangeof the desired treatment effects.

An ordinarily skilled physician, veterinarian or clinician can readilydetermine and prescribe the effective amount of the drug required toprevent, suppress or arrest the progress of diseases.

BEST MODE FOR CARRYING OUT THE INVENTION

The present invention is further described in detail with reference tothe following Examples, but the invention should in no way be restrictedthereby.

EXAMPLE 1 Preparation oftrans-3′-oxo-N-(trans-4-phenylcyclohexyl)-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

4-Phenylcyclohexylamine hydrochloride (64 mg) and1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (115 mg)were added to a solution oftrans-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-caboxylic acid(74 mg) in pyridine (2 mL). The mixture was stirred at room temperaturefor 24 hours and the reaction mixture was partitioned between water andethyl acetate. The organic layer was dried over magnesium sulfate andthe solvent was removed by evaporation. The residue was purified bypreparative thin-layer chromatography (hexane/ethyl acetate=1/1) to givethe title compound (50.7 mg) as a white solid.

¹H-NMR (300 MHz, CDCl₃, δppm): 1.72–1.89 (2H, m), 1.56–1.82 (4H, m),1.92–2.20 (8H, m), 2.28–2.40 (2H, m), 2.45–2.58 (2H, m), 3.82–3.96 (1H,m), 5.44 (1H, br d), 7.17–7.33 (5H, m), 7.52 (1H, d, J=7.8 Hz),7.58–7.69 (2H, m), 7.88 (1H, d, J=7.5 Hz).

Compounds of Examples 2 to 76 were obtained by following the sameprocedure as in Example 1, except thattrans-3′-oxospiro[cyclohexan-1,1′(3′H)-isobenzofuran]-4-carboxylic acidand 4-phenylcyclohexylamine hydrochloride used in Example 1 werereplaced with the corresponding starting materials of each desiredcompound.

EXAMPLE 2Trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, DMSO-d₆, δppm):1.69–1.77(2H, m), 1.83–2.18(8H, m),2.47–2.53(1H, m), 3.17–3.23(1H, m), 3.28–3.34(1H, m), 3.43–3.47 (1H, m),3.55–3.62(1H, m), 4.35–4.38(1H, m), 6.65–6.76(2H, m), 6.97–7.08(2H, m),7.58–7.64(2H, m), 7.77(1H, d, J=7.3 Hz), 7.83(1H, d, J=7.6 Hz), 8.17(1H,d, J=6.9 Hz).

EXAMPLE 3Trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.74–1.80(2H, m), 2.00–2.15(5H, m),2.23–2.38(3H, m), 2.48–2.52(1H, m), 3.20(1H, dd, J=9.9,3.6 Hz),3.35–3.47(2H, m), 3.59–3.65(1H, m), 4.66–4.68(1H, m), 5.73–5.77 (1H, m),6.23–6.45(3H, m), 7.17(1H, dt, J=8.2,6.9 Hz), 7.49–7.58 (2H, m),7.63–7.69(1H, m), 7.87(1H, dd, J=7.6, 0.8 Hz).

EXAMPLE 4Trans-N-[(3S)-1-(4-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.74–1.82(2H, m), 1.99–2.39(8H, m),2.48–2.52(1H, m), 3.19(1H, dd, J=9.9, 3.3 Hz), 3.26–3.34(1H, m),3.41–3.48(1H, m), 3.56(1H, dd, J=9.9, 5.9 Hz), 4.65–4.72(1H, m),5.77–5.80(1H, m), 6.48–6.54(2H, m), 6.93–7.00(2H, m), 7.49–7.58 (2H, m),7.62–7.68(1H, m), 7.88(1H, dd, J=7.6, 0.9 Hz).

EXAMPLE 5Trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CD₃OD, δppm):1.80–1.92(2H, m), 1.99–2.37(10H, m),2.60–2.70(1H, m), 3.71–3.89(4H, m), 4.04–4.20(1H, m), 7.37–7.50 (2H, m),7.52–7.64(2H, m), 7.69–7.89(4H, m).

EXAMPLE 6Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CD₃OD, δppm):1.78–1.92(2H, m), 1.98–2.38(10H, m),2.59–2.69(1H, m), 3.67–3.88(4H, m), 4.07–4.20(1H, m), 7.28(1H, dt,J=7.6,1.5 Hz), 7.43–7.68(4H, m), 7.70–7.79(2H, m), 7.84(1H, d, J=7.6Hz).

EXAMPLE 7Trans-N-[1-(4-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CD₃OD, δppm):1.77–1.93(2H, m), 1.98–2.41(10H, m),2.60–2.71(1H, m), 3.70–3.91(4H, m), 4.11–4.26(1H, m), 7.30–7.43 (2H, m),7.55–7.66(1H, m), 7.71–7.81(2H, m), 7.81–7.94(3H, m).

EXAMPLE 8Trans-3′-oxo-N-(1,2,3,4-tetrahydro-2-naphthyl)spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.70–1.91(3H, m), 1.96–2.19(5H, m),2.19–2.39(2H, m), 2.49(1H, q, J=5.0 Hz), 2.73(1H, dd, J=16.3, 7.9 Hz),2.79–3.03(2H, m), 3.15(1H, dd, J=16.3, 5.0 Hz), 4.37–4.42(1H, m),5.62(1H, br d, J=7.6 Hz), 6.99–7.21(4H, m), 7.46–7.70(3H, m), 7.86(1H,dd, J=7.6, 1.0 Hz).

EXAMPLE 9Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.61(2H, dq, J=11.6, 4.0 Hz), 1.70–1.95(2H, m), 1.95–2.23(6H, m), 2.23–2.45(2H, m), 2.53(1H, quintet, J=5.1Hz), 2.81–3.03(2H, m), 3.65(2H, brd, J=12.9 Hz), 3.90–4.07(1H, m),5.72(1H, brd, J=7.7 Hz), 6.52(1H, dt, J=8.2, 2.3 Hz), 6.58(1H, dt,J=12.3, 2.3 Hz), 6.69(1H, dt, J=8.3, 2.3 Hz), 7.17(1H, q, J=7.9 Hz),7.56(1H, dd, J=7.3, 4.6 Hz), 8.03(1H, d, J=7.9 Hz), 8.89(1H, d, J=4.6Hz).

EXAMPLE 10Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.59(2H, dq, J=11.5, 4.0 Hz), 1.70–2.60(8H,m), 2.80–3.03(2H, m), 3.55–3.79(2H, m), 3.90–4.09(1H, m), 5.63(1H, brd,J=7.9 Hz), 6.30–6.81(3H, m), 7.10–7.24(1H, m), 7.59 (1H, dd, J=5.2, 1.2Hz), 8.84(1H, d, J=5.2 Hz), 9.14(1H, s).

EXAMPLE 11Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.70(2H, m), 1.70–1.96(2H, m),1.96–2.27(6H, m), 2.27–2.61(3H, m), 2.82–3.02(2H, m), 3.57–3.78 (2H, m),3.94–4.09(1H, m), 5.64(1H, brd, J=7.9 Hz), 6.44–6.78(3H, m),7.10–7.23(1H, m), 7.77(1H, dd, J=5.0, 1.1 Hz), 8.86(1H, d, J=5.0 Hz),9.04(1H, d, J=1.1 Hz).

EXAMPLE 12Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.49–1.69(2H, m), 1.80–2.53(11H, m),2.82–3.03(2H, m), 3.53–3.78(2H, m), 3.95–4.17(1H, m), 5.70(1H, br d,J=7.6 Hz), 6.43–6.76(3H, m), 7.11–7.24(1H, m), 7.49(1H, dd, J=7.8, 4.9Hz), 8.15(1H, dd, J=7.8, 1.6 Hz), 8.84(1H, dd, J=4.9, 1.6 Hz).

EXAMPLE 13Trans-N-(6-methoxy-1,2,3,4-tetrahydro-2-naphthyl)-3-oxospiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.71–1.95(3H, m), 1.95–2.23(5H, m),2.23–2.42(2H, m), 2.50(1H, q, J=5.0 Hz), 2.66(1H, dd, J=16.0, 7.8 Hz),2.77–3.01(2H, m), 3.07(1H, dd, J=16.0, 5.0 Hz), 3.77(3H, s),4.24–4.42(1H, m), 5.96(1H, br d, J=7.7 Hz), 6.65(1H, d, J=2.5 Hz),6.72(1H, dd, J=8.4, 2.5 Hz), 6.97(1H, d, J=8.5 Hz), 7.61(1H, d, J=5.0Hz), 8.83(1H, d, J=5.0 Hz), 9.12(1H, s).

EXAMPLE 14Trans-3′-oxo-N-[(3S)-5-oxo-1-phenyl-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, DMSO-d₆, δppm):1.68–1.76(2H, m), 1.86–2.11(6H, m),2.40–2.54(2H, m), 2.92(1H, dd, J=17.1, 8.2 Hz), 3.60–3.67(1H, m),4.16(1H, dd, J=10.2, 7.0 Hz), 4.46–4.51(1H, m), 7.10–7.16(3H, m),7.33–7.40(2H, m), 7.57–7.67(4H, m), 7.74–7.84(2H, m), 8.46(1H, d, J=6.7Hz).

EXAMPLE 15Trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.80–2.00(3H, m), 2.00–2.20(4H, m),2.30–2.40(3H, m), 2.52(1H, quintet, J=5.2 Hz), 3.30–3.40(2H, m),3.50–3.70(2H, m), 4.60–4.70(1H, m), 5.94(1H, d, J=7.7 Hz), 6.65–6.80(2H,m), 6.95–7.10(2H, m), 7.70–7.80(1H, m), 8.86(1H, d, J=4.9 Hz), 9.04(1H,s).

EXAMPLE 16Trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.75–1.90(2H, m), 2.00–2.20(5H, m),2.30–2.40(3H, m), 2.51(1H, quintet, J=4.9 Hz), 3.20(1H, dd, J=10.2, 3.4Hz), 3.30–3.50(2H, m), 3.61(1H, dd, J=10.0, 6.0 Hz), 4.60–4.70 (1H, m),5.93(1H, d, J=7.2 Hz), 6.25(1H, dt, J=12.1, 2.3 Hz), 6.30–6.36 (1H, m),6.36–6.45(1H, m), 7.15(1H, dt, J=8.2, 6.9 Hz), 7.70–7.80 (1H, m),8.80–8.90(1H, m), 9.04(1H, s).

EXAMPLE 17Trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.18–1.93(2H, m), 1.49–1.74(2H, m),1.72–1.88(2H, m), 1.91–2.22(8H, m), 2.27–2.42(2H, m), 2.45–2.59 (2H, m),3.79–3.97(1H, m), 5.33–5.48(1H, m), 7.12–7.35(5H, m), 7.58 (1H, d, J=5.4Hz), 8.84(1H, d, J=5.4 Hz), 9.15(1H, s).

EXAMPLE 18Trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.15–1.41(2H, m), 1.43–1.84(2H, m),1.86–2.24(10H, m), 2.28–2.60(4H, m), 3.78–4.00(1H, m), 5.29–5.50 (1H,m), 7.08–7.37(5H, m), 7.76(1H, dd, J=4.8, 1.2 Hz), 8.86(1H, d, J=4.8Hz), 9.04(1H, d, J=1.2 Hz).

EXAMPLE 19Trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.18–1.43(2H, m), 1.43–1.77(2H, m),1.77–2.62(14H, m), 3.80–4.00(1H, m), 5.34–5.51(1H, m), 7.09–7.48 (5H,m), 7.46(1H, dd, J=7.8, 4.8 Hz), 8.17(1H, dd, J=7.8, 1.5 Hz), 8.84 (1H,dd, J=4.8, 1.5 Hz).

EXAMPLE 20Trans-3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.75–1.88(2H, m), 1.95–2.20(6H, m),2.30–2.54(4H, m), 3.20–3.62(4H, m), 4.62–4.72(1H, m), 5.70–5.80 (1H, m),6.60(2H, d, J=8.7 Hz), 6.74(1H, t, J=7.4 Hz), 7.20–7.32(2H, m), 7.76(1H,d, J=5.0 Hz), 8.87(1H, d, J=5.0 Hz), 9.04(1H, s).

EXAMPLE 21Trans-3-oxo-N-[(3S)-1-(3-trifluoromethylphenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(200 MHz, CDCl₃, δppm):1.75–2.57(11H, m), 3.18–3.71(4H, m),4.62–4.78(1H, m), 5.68–5.80(1H, m), 6.68–6.80(2H, m), 6.90–7.00 (1H, m),7.25–7.38(1H, m), 7.76(1H, d, J=5.0 Hz), 8.87(1H, d, J=5.0 Hz), 9.04(1H,s).

EXAMPLE 22Trans-3-oxo-N-[(3S)-1-(2-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.70–1.90(2H, m), 2.00–2.20(5H, m),2.20–2.40(3H, m), 2.51(1H, quintet, J=4.9 Hz), 3.00–3.10(2H, m),3.42(1H, dd, J=10.9, 3.6 Hz), 3.77(1H, dd, J=10.9, 5.9 Hz), 4.60–4.70(1H, m), 5.83(1H, d, J=7.3 Hz), 6.38(1H, d, J=8.6 Hz), 6.55–6.65(1H, m),7.64(1H, ddd, J=9.0,7.0,2.0 Hz), 7.56(1H, dd, J=5.4, 1.6 Hz),8.10–8.20(1H, m), 8.84(1H, d, J=5.4 Hz), 9.14(1H, s).

EXAMPLE 23Trans-3-oxo-N-[(3S)-1-(3-pyridyl)-3-pyrrolidinyl]spiro[5-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

H-NMR(300 MHz, CDCl₃, δppm):1.70–1.90(2H, m), 2.00–2.20(5H, m),2.25–2.45(3H, m), 2.54(1H, quintet, J=5.3 Hz), 3.23(1H, dd, J=9.9, 3.0Hz), 3.30–3.50(2H, m), 3.63(1H, dd, J=9.7, 5.9 Hz), 4.60–4.70 (1H, m),6.17(1H, d, J=7.2 Hz), 6.70–6.90(1H, m), 7.00–7.20(1H, m), 7.57(1H, dd,J=5.3, 0.9 Hz), 7.90–8.00(2H, m), 8.85(1H, d, J=5.3 Hz), 9.15(1H, s).

EXAMPLE 24Trans-N-[trans-4-(4-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.13–1.41(2H, m), 1.41–1.68(2H, m),1.72–2.26(10H, m), 2.26–2.60(4H, m), 3.78–4.00(1H, m), 5.32–5.51 (1H,m), 6.81–7.07(2H, m), 7.07–7.37(2H, m), 7.76(1H, dd, J=5.4, 1.2 Hz),8.86(1H, d, J=5.4 Hz), 9.04(1H, d, J=1.2 Hz).

EXAMPLE 25Trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.19–1.41(2H, m), 1.49–1.73(2H, m),1.73–2.27(10H, m), 2.39–2.70(4H, m), 3.79–4.00(1H, m), 5.32–5.48 (1H,m), 6.82–7.03(3H, m), 7.19–7.34(1H, m), 7.76(1H, dd, J=4.8, 0.9 Hz),8.86(1H, d, J=4.8 Hz), 9.04(1H, d, J=0.9 Hz).

EXAMPLE 26Trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.19–1.41(2H, m), 1.49–1.73(2H, m),1.73–2.25(10H, m), 2.25–2.42(2H, m), 2.42–2.60(2H, m), 3.77–3.96 (1H,m), 5.36–5.56(1H, m), 6.82–7.03(1H, m), 7.19–7.34(1H, m), 7.54 (1H, dd,J=7.8, 4.5 Hz), 8.03(1H, d, J=7.8 Hz), 8.88(1H, d, J=4.5 Hz).

EXAMPLE 27Trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxospiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.19–1.41(2H, m), 1.49–1.76(2H, m),1.78–2.60(14H, m), 3.80–4.00(1H, m), 5.35–5.53(1H, m), 6.82–7.03 (3H,m), 7.18–7.35(1H, m), 7.46(1H, dd, J=7.8, 4.8 Hz), 8.17(1H, dd, J=7.8,1.5 Hz), 8.84(1H, dd, J=4.8, 1.5 Hz).

EXAMPLE 28Trans-N-[(3S)-1-(3,5-difluorophenyl)-3-pyrrolidinyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.80–1.90(2H, m), 1.95–2.20(5H, m),2.30–2.45(3H, m), 2.53(1H, quintet, J=4.6 Hz), 3.10–3.20(1H, m),3.30–3.50(2H, m), 3.60–3.70(1H, m), 4.60–4.70(1H, m), 5.60–5.70 (1H, m),6.50–6.60(2H, m), 6.60–6.70(1H, m), 7.76(1H, d, J=4.9 Hz), 8.87(1H, d,J=4.9 Hz), 9.03(1H, s).

EXAMPLE 29Trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.45–1.61(2H, m), 1.78–1.90(2H, m),2.00–2.21(6H, m), 2.31–2.45(2H, m), 2.45–2.55(1H, m), 2.88–3.00 (2H, m),3.60–3.71(2H, m), 3.95–4.10(1H, m), 5.48(1H, br d, J=7.5 Hz),6.18–6.29(1H, m), 6.29–6.43(2H, m), 7.77(1H, dd, J=5.0, 1.1 Hz),8.86(1H, d, J=5.0 Hz), 9.03(1H, d, J=1.1 Hz).

EXAMPLE 30Trans-N-[3-(3-fluorophenyl)-tetrahydropyran-6-yl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.43–2.10(13H, m), 3.24(1H, t, J=10.5 Hz),4.02–4.20(1H, m), 4.24(1H, d, J=10.5 Hz), 4.32(1H, d, J=10.5 Hz),5.20–5.40(1H, m), 6.88–7.03(1H, m), 7.03–7.16(2H, m), 7.20–7.39(1H, m),7.76(1H, dd, J=5.1, 1.2 Hz), 8.87(1H, d, J=5.1 Hz), 9.04 (1H, d, J=1.2Hz).

EXAMPLE 31Trans-N-[trans-4-(2-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.22–1.46(2H, m), 1.52–2.28(12H, m),2.28–2.60(3H, m), 2.76–2.97(1H, m), 3.80–4.00(1H, m), 5.35–5.53 (1H, m),6.92–7.41(4H, m), 7.76(1H, dd, J=4.8, 1.2 Hz), 8.86(1H, d, J=4.8 Hz),9.04(1H, d, J=1.2 Hz).

EXAMPLE 32Trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.74(2H, m), 1.60–2.10(5H, m),2.16–2.27(1H, m), 2.39–2.47(1H, m), 2.68–2.75(2H, m), 2.86(2H, d, J=6.6Hz), 3.79(2H, s), 4.28–4.39(1H, m), 5.85(1H, d, J=8.4 Hz),7.13–7.37(10H, m), 7.46(1H, d, J=8.1 Hz), 7.51(1H, d, J=7.8 Hz),7.63(1H, t, J=7.8 Hz), 7.86(1H, d, J=7.8 Hz).

EXAMPLE 33Trans-N-benzhydryl-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(200 MHz, CDCl₃, δppm):1.70–1.80(2H, m), 2.10–2.40(6H, m),2.64(1H, quintet, J=4.9 Hz), 6.16(1H, d, J=7.6 Hz), 6.28(1H, d, J=7.6Hz), 7.20–7.40(10H, m), 7.45–7.55(2H, m), 7.60–7.70(1H, m),7.80–7.90(1H, m).

EXAMPLE 34Trans-1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.70(4H, m), 1.71–1.83(2H, m),1.95–2.15(6H, m), 2.30–2.40(1H, m), 2.82–2.96(2H, m), 2.89(3H, s),3.60–3.68(2H, br d, J=12.9 Hz), 3.72(2H, s), 3.92–4.08(1H, m), 5.47(1H,d, J=7.7 Hz), 6.85(1H, t, J=7.3 Hz), 6.94(2H, d, J=8.5 Hz), 7.05(1H, t,J=7.3 Hz), 7.18–7.30(3H, m), 7.40(2H, t, J=7.3 Hz).

EXAMPLE 35Trans-N-(2-indanyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.63(2H, m), 1.68–1.80(2H, m),1.99–2.11(4H, m), 2.23–2.32(1H, m), 2.81(2H, dd, J=16.2, 4.2 Hz),2.88(3H, s), 3.36(2H, dd, J=16.2, 7.2 Hz), 3.70(2H, s), 4.72–4.85 (1H,m), 5.68–5.77(1H, m), 7.05(1H, t, J=7.2 Hz), 7.18–7.30(5H, m),7.34–7.45(2H, m).

EXAMPLE 36Trans-N-[1-(3-fluorophenyl)-4-piperidyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.46–1.68(4H, m), 1.70–1.84(2H, m),2.00–2.13(6H, m), 2.30–2.40(1H, m), 2.89(3H, s), 2.86–2.98(2H, m),3.61–3.71(2H, m), 3.72(2H, s), 3.95–4.05(1H, m), 5.43(1H, d, J=7.7 Hz),6.49(1H, dt, J=8.2, 2.3 Hz), 6.60(1H, dt, J=12.4, 2.3 Hz), 6.68 (1H, dd,J=8.2, 2.3 Hz), 7.05(1H, dt, J=7.6, 1.1 Hz), 7.17(1H, t, J=7.6 Hz),7.22(1H, dt, J=7.6, 1.3 Hz), 7.40(1H, dd, J=7.6, 1.1 Hz), 7.42 (1H, dd,J=7.6, 1.1 Hz).

EXAMPLE 37Trans-1-methanesulfonyl-N-[1-(2-pyridyl)-4-piperidyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.38–1.54(2H, m), 1.53–1.63(2H, m),1.65–1.75(4H, m), 2.00–2.12(6H, m), 2.29–2.40(1H, m), 2.88(3H, s),3.02(2H, ddd, J=13.8, 11.2, 2.5 Hz), 3.72(2H, s), 4.06(1H, m), 4.25 (2H,m), 5.44(1H, d, J=7.8 Hz), 6.56–6.66(1H, m), 6.68(1H, d, J=8.7 Hz),7.05(1H, dt, J=7.6, 1.0 Hz), 7.22(1H, dt, J=7.6, 1.2 Hz), 7.39 (1H, d,J=7.6 Hz), 7.42(1H, dd, J=7.6, 1.0 Hz), 7.47(1H, ddd, J=8.8, 7.1, 2.0Hz), 8.13–8.24(1H, m).

EXAMPLE 38Trans-1-methanesulfonyl-N-(1-phenyl-3-piperidyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.54–1.88(8H, m), 2.00–2.19(4H, m),2.33–2.42(1H, m), 2.89(3H, s), 2.96–3.05(1H, m), 3.13–3.43(3H, m),3.68–3.75(2H, m), 4.20–4.30(1H, m), 6.03–6.10(1H, m), 6.88(1H, t, J=7.2Hz), 6.91–6.99(2H, m), 7.01–7.08(1H, m), 7.19–7.30(3H, m), 7.37–7.43(2H,m).

EXAMPLE 39Trans-N-[1-(3,5-difluorophenyl)-3-piperidyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.53–1.90(8H, m), 2.00–2.13(4H, m),2.33–2.42(1H, m), 2.88(3H, s), 3.01–3.20(3H, m), 3.40–3.48(1H, m),3.67–3.82(2H, m), 4.10–4.21(1H, m), 5.97–6.03(1H, m), 6.19–6.28 (1H, m),6.35–6.45(2H, m), 7.05(1H, t, J=7.5 Hz), 7.22(1H, t, J=7.5 Hz), 7.38(1H,d, J=7.8 Hz), 7.42(1H, d, J=7.8 Hz).

EXAMPLE 40Trans-1-methanesulfonyl-N-[1-(2-pyridyl)-3-piperidyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.90(8H, m), 1.95–2.32(4H, m),2.31–2.40(1H, m), 2.88(3H, s), 3.43–3.50(1H, m), 3.70(2H, s),3.55–3.74(3H, m), 4.08–4.16(1H, m), 6.30(1H, d, J=7.6 Hz), 6.61(1H, dd,J=7.1, 5.0 Hz), 6.73(1H, d, J=8.6 Hz), 7.03(1H, dt, J=7.5, 1.1 Hz), 7.21(1H, dt, J=7.5, 1.1 Hz), 7.38(2H, d, J=8.6 Hz), 7.47(1H, ddd, J=8.6,7.1, 2.0 Hz), 8.14(1H, dd, J=5.0, 2.0 Hz).

EXAMPLE 41Trans-1-methanesulfonyl-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.52–1.82(6H, m), 1.96–2.13(3H, m),2.28–2.40(2H, m), 2.87(3H, m), 3.22(1H, dd, J=9.9, 3.3 Hz),3.31–3.51(2H, m), 3.59(1H, dd, J=9.9, 5.7 Hz), 3.67–3.72(2H, m),4.61–4.71(1H, m), 5.82–5.89(1H, m), 6.60(2H, d, J=7.8 Hz), 6.73(1H, t,J=7.5 Hz), 7.04(1H, dd, J=7.5, 1.2 Hz), 7.20–7.29(3H, m), 7.40(2H, t,J=8.4 Hz).

EXAMPLE 42 Trans-1-methanesulfonyl-N-[(3R)-1-phenyl-3-pyrrolidinylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.52–1.82(6H, m), 1.96–2.13(3H, m),2.28–2.40(2H, m), 2.87(3H, m), 3.22(1H, dd, J=9.9, 3.3 Hz),3.31–3.51(2H, m), 3.59(1H, dd, J=9.9, 5.7 Hz), 3.67–3.72(2H, m),4.61–4.71(1H, m), 5.82–5.89(1H, m), 6.60(2H, d, J=7.8 Hz), 6.73(1H, t,J=7.5 Hz), 7.04(1H, dd, J=7.5, 1.2 Hz), 7.20–7.29(3H, m), 7.40(2H, t,J=8.4 Hz).

EXAMPLE 43Trans-1-methanesulfonyl-N-(2-phenylcyclopropyl)spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.10–1.30(2H, m), 1.50–1.87(4H, m),1.95–2.20(5H, m), 2.30–2.38(1H, m), 2.89(3H, s), 2.86–2.95(1H, m),3.72(2H, s), 5.75–5.84(1H, m), 6.99–7.48(9H, m).

EXAMPLE 44Trans-1-methanesulfonyl-N-[2-(3-pyridyl)cyclo-propyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.20–1.34(2H, m), 1.52–1.89(4H, m),2.00–2.20(5H, m), 2.34–2.43(1H, m), 2.89(3H, s), 2.87–2.94(1H, m),3.72(2H, s), 5.86–5.95(1H, m), 7.05(1H, dt, J=7.5, 1.1 Hz),7.19–7.30(2H, m), 7.37–7.47(2H, m), 7.51(1H, brd, J=7.9 Hz), 8.45(1H,dd, J=4.7 Hz, 1.7 Hz), 8.50(1H, d, J=2.1 Hz).

EXAMPLE 45Trans-N-[(S)-1-benzyl-2-(benzylamino)ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.46–1.75(4H, m), 1.82–2.05(4H, m),2.25–2.34(1H, m), 2.68–2.72(2H, m), 2.88(3H, s), 2.80–2.90(2H, m),3.70(2H, s), 3.77(2H, s), 4.25–4.36(1H, m), 5.85(1H, d, J=7.5 Hz),7.03(1H, t, J=7.5 Hz), 7.15–7.32(12H, m), 7.38(1H, d, J=7.5 Hz).

EXAMPLE 46Trans-N-[1-benzylcarbamoyl-2-(4-pyridyl)ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.45–2.02(8H, m), 2.30–2.40(1H, m),2.88(3H, s), 3.00–3.19(2H, m), 3.68(2H, s), 4.28–4.43(2H, m), 4.78 (1H,q, J=7.5 Hz), 6.40–6.52(2H, m), 6.98–7.40(11H, m), 8.46(2H, d, J=5.9Hz).

EXAMPLE 47Trans-N-[2-(4-fluorophenyl)-1-[(4-pyridyl-methyl)carbamoyl]ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.45–2.10(8H, m), 2.35–2.45(1H, m),2.88(3H, s), 3.00–3.18(2H, m), 3.70(2H, s), 4.31(1H, dd, J=15.8, 6.0Hz), 4.41(1H, dd, J=15.8, 6.0 Hz), 4.76(1H, q, J=7.9 Hz), 6.42(1H, d,J=7.9 Hz), 6.79(1H, t, J=6.0 Hz), 6.90–7.10(5H, m), 7.11–7.32(4H, m),7.38(1H, d, J=8.0 Hz), 8.47(2H, d, J=5.3 Hz).

EXAMPLE 48Trans-N-(2-hydroxy-2-phenylethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.63(2H, m), 1.67–1.82(2H, m),1.92–2.12(4H, m), 2.33–2.42(1H, m), 2.89(3H, s), 3.27–3.47(2H, m),3.71(2H, s), 3.72–3.82(1H, m), 4.88–4.94(1H, m), 5.91–6.02(1H, m),7.05(1H, t, J=7.8 Hz), 7.19–7.41(8H, m).

EXAMPLE 49Trans-N-(benzoylmethyl)-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.59–1.70(2H, m), 1.80–1.91(2H, m),2.02–2.21(4H, m), 2.51–2.60(1H, m), 2.90(3H, s), 3.76(2H, s), 4.81 (2H,d, J=4.2 Hz), 6.60–6.70(1H, m), 7.04(1H, t, J=7.5 Hz), 7.22(1H, t, J=7.5Hz), 7.38–7.43(2H, m), 7.52(2H, t, J=7.5 Hz), 7.64(1H, t, J=7.5 Hz),8.00(2H, d, J=6.6 Hz).

EXAMPLE 50Trans-N-[(S)-1-benzyl-2-(N-benzylmethylamino)ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.78(4H, m), 1.80–2.10(4H, m),2.23(3H, s), 2.28–2.46(3H, m), 2.88(3H, s), 2.92(2H, d, J=6.6 Hz),3.46(1H, d, J=13.2 Hz), 3.53(1H, d, J=13.2 Hz), 3.71(2H, s),4.25–4.38(1H, m), 5.62(1H, d, J=6.6 Hz), 7.02(1H, t, J=7.5 Hz),7.12–7.34 (12H, m), 7.38(1H, d, J=7.5 Hz).

EXAMPLE 51Trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-phenylethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.45–2.10(8H, m), 2.33–2.46(1H, m),2.75(3H, s), 2.88(3H, s), 3.00–3.10(2H, m), 3.69(2H, s), 4.46(1H, d,J=14.4 Hz), 4.63(1H, d, J=14.4 Hz), 5.20–5.35(1H, m), 6.75(1H, d, J=7.5Hz), 7.00–7.36(13H, m), 7.39(1H, d, J=7.5 Hz).

EXAMPLE 52Trans-N-[(S)-1-(N-benzylmethylcarbamoyl)-2-(3-pyridyl)ethyl]-1-methanesulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.45–2.08(8H, m), 2.30–2.45(1H, m),2.88(3H, s), 2.97(3H, s), 2.95–3.02(1H, m), 3.12(1H, dd, J=13.6, 7.2Hz), 3.70(2H, s), 4.45–4.62(2H, m), 5.20–5.30(1H, m), 6.60(1H, br s),7.00–7.48(11H, m), 8.45(1H, d, J=1.8 Hz), 8.47(1H, dd, J=5.1, 1.8 Hz).

EXAMPLE 53Trans-N-(4-dimethylaminophenethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.49–1.80(4H, m), 1.94–2.09(4H, m),2.22–2.33(1H, m), 2.75(2H, t, J=6.6 Hz), 2.88(3H, s), 2.92(6H, s),3.52(2H, dt, J=6.6, 6.2 Hz), 3.70(2H, s), 5.51(1H, t, J=6.2 Hz), 6.70(2H, d, J=8.8 Hz), 7.04(1H, t, J=8.1 Hz), 7.07(2H, d, J=8.8 Hz), 7.22(1H, t, J=8.1 Hz), 7.39(2H, d, J=8.1 Hz).

EXAMPLE 54Trans-1-methanesulfonyl-N-[2-(3-quinolyl)ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.49–1.79(4H, m), 1.92–2.09(4H, m),2.25–2.36(1H, m), 2.88(3H, s), 3.07(2H, t, J=6.6 Hz), 3.65(1H, dt,J=6.7, 6.6 Hz), 3.69(1H, dd, J=6.7, 6.6 Hz), 3.69(2H, s), 5.63(1H, t,J=6.7 Hz), 7.02(1H, t, J=7.3 Hz), 7.22(1H, t, J=7.3 Hz), 7.33(1H, d,J=7.3 Hz), 7.38(1H, d, J=7.3 Hz), 7.54(1H, t, J=7.9 Hz), 7.69(1H, t,J=7.9 Hz), 7.77(1H, d, J-7.9 Hz), 7.99(1H, d, J=2.2 Hz), 8.08(1H, d,J=7.9 Hz), 8.79(1H, d, J=2.2 Hz).

EXAMPLE 55Trans-N-[2-(4-dimethylaminophenyl)-2-hydroxyethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.49–1.82(4H, m), 1.98–2.12(4H, m),2.32–2.42(1H, m), 2.63–2.70(1H, m), 2.89(3H, s), 2.94(6H, s),3.35–3.45(1H, m), 3.71(2H, s), 3.60–3.78(1H, m), 4.72–4.80(1H, s),5.90–5.98(1H, m), 6.65–6.75(2H, m), 7.00–7.09(1H, m), 7.18–7.30(3H, m),7.35–7.45(2H, m).

EXAMPLE 56Trans-N-[2-hydroxy-2-(3-quinolyl)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.50–1.82(4H, m), 1.92–2.10(4H, m),2.32–2.45(1H, m), 2.88(3H, s), 3.48–3.60(2H, m), 3.69(2H, s),3.82–3.95(1H, m), 4.19–4.30(1H, m), 5.12–5.20(1H, m), 7.04(1H, t, J=7.8Hz), 7.23(1H, t, J=7.8 Hz), 7.33(1H, d, J=7.8 Hz), 7.38(1H, d, J=7.8Hz), 7.55(1H, t, J=7.8 Hz), 7.71(1H, t, J=7.8 Hz), 7.80(1H, d, J=7.8Hz), 8.10(1H, d, J=7.8 Hz), 8.21(1H, d, J=2.4 Hz), 8.88(1H, d, J=2.4Hz).

EXAMPLE 57Trans-N-[2-(3,5-difluorophenyl)-2-hydroxyethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.51–2.32(4H, m), 1.94–2.01(4H, m),2.35–2.46(1H, s), 2.89(3H, s), 3.31–3.42(1H, m), 3.71(2H, s),3.70–3.82(1H, m), 3.98(1H, d, J=4.3 Hz), 4.87–4.94(1H, m), 5.98(1H, t,J=3.0 Hz), 6.68–6.76(1H, m), 6.87–6.98(2H, m), 7.06(1H, t, J=7.7 Hz),7.23(1H, t, J=7.7 Hz), 7.32–7.41(2H, m).

EXAMPLE 58Trans-N-[(S)-1-benzyl-2-[(3-pyridylmethyl)amino]ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.45–1.75(4H, m), 1.80–2.09(4H, m),2.25–2.38(1H, m), 2.70(2H, d, J=7.5 Hz), 2.86(3H, s), 2.84–2.90(2H, m),3.69(2H, s), 3.78(2H, s), 4.25–4.40(1H, m), 5.70(1H, d, J=7.5 Hz),7.03(1H, dd, J=7.5, 2.4 Hz), 7.12–7.40(9H, m), 7.57–7.63(1H, m),8.50(1H, dd, J=5.1, 1.5 Hz), 8.55(1H, d, J=1.5 Hz).

EXAMPLE 59Trans-N-[(S)-1-benzyl-2-[(2-pyridylmethyl)amino]ethyl]-1-methylsulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.45–2.10(8H, m), 2.30–2.40(1H, m),2.66–2.76(2H, m), 2.88(3H, s), 2.80–2.99(2H, m), 3.70(2H, s), 3.90 (2H,dd, J=14.4, 5.7 Hz), 4.23–4.37(1H, m), 6.14(1H, d, J=7.5 Hz), 7.02(1H,t, J=7.5 Hz), 7.12–7.30(9H, m), 7.36(1H, t, J=7.5 Hz), 7.62 (1H, dt,J=7.5, 2.1 Hz), 8.54(1H, dd, J=5.1, 2.1 Hz).

EXAMPLE 60Trans-N-[(S)-2-anilino-1-benzylethyl]-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.42–2.07(8H, m), 2.24–2.33(1H, m),2.87(3H, s), 2.84–2.91(1H, m), 3.00(1H, dd, J=14.1, 6.3 Hz), 3.20 (1H,dd, J=12.4, 7.5 Hz), 3.33(1H, dd, J=12.4, 4.5 Hz), 3.67(2H, s),4.47–4.58(1H, m), 5.49(1H, d, J=7.5 Hz), 6.60(1H, d, J=7.5 Hz), 6.70(1H, t, J=7.5 Hz), 7.00(1H, t, J=7.5 Hz), 7.12–7.40(10H, m).

EXAMPLE 61Trans-N-[(S)-1-benzyl-2-(isobutylamino)ethyl]-1-methane-sulfonylspiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):0.89(6H, d, J=6.3 Hz), 1.45–2.10(9H, m),2.30–2.40(1H, m), 2.43(2H, d, J=6.3 Hz), 2.65–2.78(2H, m), 2.88 (3H, s),2.80–2.93(2H, m), 3.70(2H, s), 4.22–4.35(1H, m), 6.02(1H, d, J=7.5 Hz),7.15–7.40(9H, m).

EXAMPLE 62Trans-1-methanesulfonyl-N-[2-phenyl-1-(methoxy-carbonyl)ethyl]spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.49–1.60(2H, m), 1.63–1.78(2H, m),1.87–2.10(4H, m), 2.33–2.41(1H, m), 2.88(3H, s), 3.10(1H, dd, J=14.1,6.3 Hz), 3.22(1H, dd, J=14.1, 5.7 Hz), 3.71(2H, s), 3.77(3H, s),4.91–4.97(1H, m), 5.95(1H, br d, J=7.8 Hz), 7.04(1H, t, J=6.9 Hz),7.11(2H, d, J=6.3 Hz), 7.19–7.40(6H, m).

EXAMPLE 63Trans-N-(1-hydroxymethyl-2-phenylethyl)-1-methanesulfonyl-spiro[indoline-3,1′-cyclohexane]-4′-carboxamide

¹H-NMR(200 MHz, CDCl₃, δppm):1.43–2.11(7H, m), 2.29–2.40(1H, m),2.52–2.67(1H, m), 2.79–3.02(2H, m), 2.88(3H, s), 3.59–3.81(2H, m),3.69(2H, s), 4.18–4.35(1H, m), 5.69–5.81(1H, m), 7.04(1H, dt, J=7.6, 1.2Hz), 7.18–7.41(8H, m).

EXAMPLE 64Trans-N-[1-(3-trifluoromethylphenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.56–1.65(2H, m), 1.80–1.88(2H, m),2.04–2.21(6H, m), 2.35–2.44(2H, m), 2.50–2.53(1H, m), 2.91–3.00 (2H, m),3.62–3.73(2H, m), 4.00–4.16(1H, m), 5.58–5.60(1H, m), 7.06–7.13(3H, m),7.27–7.37(4H, m), 7.76(1H, d, J=3.7 Hz), 8.87(1H, d, J=4.9 Hz), 9.04(1H,s).

EXAMPLE 65Trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.18–1.31(2H, m), 1.70–1.82(2H, m),2.00–2.21(5H, m), 2.22–2.38(2H, m), 2.46–2.56(1H, m), 2.89–2.98 (1H, m),6.89(1H, br s), 6.83–6.91(2H, m), 6.97(1H, d, J=7.2 Hz), 7.19–7.29(1H,m), 7.52(1H, t, J=7.2 Hz), 7.55–7.69(2H, m), 7.87(1H, d, J=7.8 Hz).

EXAMPLE 66Trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.12–1.28(2H, m), 1.71–1.82(2H, m),1.99–2.20(5H, m), 2.21–2.38(2H, m), 2.46–2.54(1H, m), 2.81–2.90 (1H, m),5.86(1H, br s), 6.98(2H, t, J=8.7 Hz), 7.13–7.21(2H, m), 7.52(1H, t,J=7.2 Hz), 7.58–7.70(2H, m), 7.88(1H, d, J=7.8 Hz).

EXAMPLE 67Trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran]-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.56–1.74(2H, m), 1.78–1.90(2H, m),2.01–2.23(6H, m), 2.32–2.48(2H, m), 2.48–2.57(1H, m), 2.77–2.90 (2H, m),3.38–3.50(2H, m), 3.90–4.07(1H, m), 5.51(1H, m), 6.90–7.10 (4H, m),7.74(1H, d, J=5.0 Hz), 8.87(1H, d, J=5.0 Hz), 9.05(1H, s).

EXAMPLE 68Trans-3′-oxo-N-[5-oxo-1-(2-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.68–1.81(2H, m), 1.96–2.15(4H, m),2.15–2.30(2H, m), 2.43–2.54(2H, m), 2.99(1H, dd, J=17.4, 7.6 Hz),3.73(1H, dd, J=10.6, 2.4 Hz), 4.16(1H, dd, J=10.6, 6.0 Hz), 4.65–4.76(1H, m), 6.80(1H, br s), 7.09–7.21(2H, m), 7.23–7.32(1H, m),7.32–7.42(1H, m), 7.47–7.57(2H, m), 7.59–7.68(1H, m), 7.88(1H, d, J=7.5Hz).

EXAMPLE 69Trans-3′-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.71–1.94(2H, m), 2.01–2.34(6H, m),2.52–2.64(2H, m), 2.98–3.11(1H, m), 3.77(1H, dd, J=10.5, 2.9 Hz),4.23(1H, dd, J=10.5, 6.4 Hz), 4.65–4.77(1H, m), 6.78–7.13(2H, m),7.17–7.33(2H, m), 7.42–7.69(4H, m), 7.80–7.88(1H, m).

EXAMPLE 70Trans-3-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.76–1.91(2H, m), 2.06–2.23(4H, m),2.25–2.40(2H, m), 2.50–2.62(2H, m), 3.07(1H, dd, J=17.6, 8.1 Hz),3.77(1H, dd, J=10.7, 2.4 Hz), 4.24(1H, dd, J=10.6, 6.2 Hz), 4.67–4.79(1H, m), 6.79–6.92(2H, m), 7.16–7.35(2H, m), 7.46–7.54(1H, m), 7.75 (1H,d, J=5.0 Hz), 8.87(1H, d, J=5.0 Hz), 9.04(1H, s).

EXAMPLE 71Trans-N-[trans-4-(3-trifluoromethylphenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.26–1.40(2H, m), 1.59–1.72(2H, m),1.80–1.88(2H, m), 1.97–2.20(7H, m), 2.36–2.63(4H, m), 3.88–3.93 (1H, m),5.42(1H, d, J=8.4 Hz), 7.40–7.47(4H, m), 7.76(1H, d, J=6.0 Hz), 8.87(1H,d, J=4.9 Hz), 9.04(1H, s).

EXAMPLE 72Trans-3′-oxo-N-[2-oxo-1-phenyl-4-piperidyl]spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.65–1.85(1H, m), 1.95–2.20(5H, m),2.20–2.40(3H, m), 2.43–2.60(2H, m), 2.92–3.00(1H, m), 3.60–3.80 (2H, m),4.40–4.45(1H, m), 5.68–5.70(1H, m), 7.20–7.23(3H, m), 7.38–7.42(2H, m),7.45–7.56(2H, m), 7.62–7.66(1H, m), 7.86–7.87(1H, m).

EXAMPLE 73Trans-3′-oxo-N-[2-oxo-1-(3-fluorophenyl)-4-piperidyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.60–1.90(1H, m), 1.95–2.20(5H, m),2.22–2.60(5H, m), 2.96–3.00(1H, m), 3.62–3.80(2H, m), 4.38–4.50 (1H, m),5.70–5.80(1H, m), 7.20–7.30(4H, m), 7.40–7.42(2H, m), 7.72–7.80(1H, m),8.84–8.85(1H, m), 9.01(1H, s).

EXAMPLE 74Trans-N-[trans-2-(2-fluorophenyl)cyclopropyl]-3′-oxospiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.20–1.37(2H, m), 1.70–1.82(2H, m),2.01–2.38(7H, m), 2.48–2.57(1H, m), 3.00–3.09(1H, m), 5.92(1H, br s),6.99–7.21(4H, m), 7.51(1H, t, J=7.2 Hz), 7.56–7.69(2H, m), 7.87 (1H, d,J=7.5 Hz).

EXAMPLE 75Trans-N-[trans-2-(3-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.17–1.32(2H, m), 1.75–1.89(2H, m),2.00–2.25(5H, m), 2.31–2.58(3H, m), 2.89–2.99(1H, m), 5.84(1H, br s),6.80–7.03(3H, m), 7.20–7.32(1H, m), 7.76((1H, dd, J=5.1, 0.9 Hz),8.87(1H, d, J=5.1 Hz), 9.03(1H, d, J=0.9 Hz).

EXAMPLE 76Trans-N-[trans-2-(4-fluorophenyl)cyclopropyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.12–1.30(2H, m), 1.78–1.90(2H, m),2.01–2.22(5H, m), 2.31–2.48(2H, m), 2.48–2.57(1H, m), 2.82–2.91 (1H, m),5.84(1H, br s), 6.98(2H, t, J=8.7 Hz), 7.12–7.22(2H, m), 7.76(1H, dd,J=4.8, 1.2 Hz), 8.87(1H, d, J=4.8 Hz), 9.04(1H, s).

EXAMPLE 77 Preparation of1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

(1) Preparation of phenyl N-(1-phenyl-4-piperidyl)carbamate

Pyridine (24 μL) and phenyl chlorocarbonate (32 μL) were added to asolution of 1-phenyl-4-piperidylamine (35 mg) in tetrahydrofuran (1 mL),and the mixture was stirred at room temperature for 12 hours. Thereaction mixture was poured into saturated aqueous sodium bicarbonate,and extracted with ethyl acetate. The organic layer was dried overanhydrous magnesium sulfate and concentrated. The residue was purifiedby column chromatography on silica gel (ethyl acetate/chloroform=1/1) togive the title compound (37 mg).

(2) Preparation of1-methanesulfonyl-N-(1-phenyl-4-piperidyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

1-Methanesulfonyl-spiro[indoline-3,4′-piperidine] hydrochloride (37 mg)and triethylamine (170 μL) were added to a solution of phenylN-(1-phenyl-4-piperidyl)carbamate (36 mg) in chloroform (3 mL), and themixture was heated to reflux for 15 hours. The reaction mixture waspoured into saturated aqueous sodium bicarbonate and extracted withethyl acetate. The organic layer was dried over anhydrous magnesiumsulfate and concentrated. The residue was crystallized from diethylether to give the title compound (18 mg) as a colorless crystal.

¹H-NMR(300 MHz, CDCl₃, δppm):1.49–2.13(12H, m), 2.71–2.83(1H, m),2.84–3.00(2H, m), 2.92(3H, s), 3.10–3.19(1H, m), 3.60–3.70(1H, m),3.85(2H, s), 3.90–4.01(1H, m), 4.37(1H, d, J=7.8 Hz), 6.84(1H, t, J=7.2Hz), 6.94(1H, d, J=8.7 Hz), 7.07(1H, t, J=7.2 Hz), 7.11–7.29(5H, m),7.40(1H, d, J=8.4 Hz).

Compounds of Examples 78 to 83 were obtained by following the sameprocedure as in Example 77-(2), except that phenylN-(1-phenyl-4-piperidyl)carbamate and1-methanesulfonylspiro[indoline-3,4′-piperidine]hydrochloride used inExample 77-(2) were replaced with the corresponding starting material ofeach desired compound.

EXAMPLE 783-Oxo-N-(1-phenyl-3-piperidyl)spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.60–1.90(2H, m), 2.04–2.18(2H, m),2.53–2.60(1H, m), 3.01–3.49(9H, m), 3.92–4.20(3H, m), 5.03(1H, d, J=7.8Hz), 6.88(1H, t, J=7.5 Hz), 6.97(2H, d, J=7.5 Hz), 7.21–7.30(2H, m),7.35(1H, d, J=7.8 Hz), 7.54(1H, t, J=7.5 Hz), 7.68(1H, t, J=7.5 Hz),7.88(1H, d, J=7.5 Hz).

EXAMPLE 793-Oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[isobenzofuran-1(3H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.98–2.20(3H, m), 2.30–2.41(1H, m),2.99–3.10(2H, m), 3.22–3.40(4H, m), 3.42–3.53(1H, m), 3.59–3.65 (1H, m),3.96–4.11(2H, m), 4.53–4.64(1H, m), 4.68–4.77(1H, m), 6.60 (2H, d, J=7.8Hz), 6.72(1H, t, J=7.5 Hz), 7.25(2H, t, J=7.5 Hz), 7.37 (1H, d, J=7.5Hz), 7.55(1H, t, J=7.5 Hz), 7.69(1H, t, J=7.5 Hz), 7.89 (1H, d, J=7.8Hz).

EXAMPLE 80N-[1-Benzylcarbamoyl-2-cyclohexylethyl]-3,4-dihydro-3-oxo-spiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):0.88–1.03(2H, m), 1.10–1.25(3H, m),1.27–1.45(1H, m), 1.50–1.86(8H, m), 2.03–2.19(2H, m), 3.05–3.19 (2H, m),3.66(2H, s), 3.94–4.05(2H, m), 4.34–4.43(2H, m), 4.52(1H, dd, J=13.5,6.0 Hz), 5.10(1H, d, J=7.5 Hz), 6.60(2H, br s), 7.15–7.37(9H, m).

EXAMPLE 81N-[(S)-1-Benzyloxymethyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):0.80–1.32(7H, m), 1.40–1.50(2H, m),1.60–1.85(6H, m), 2.03–2.20(2H, m), 3.02–3.18(2H, m), 3.47(1H, dd,J=9.7, 3.3 Hz), 3.54(1H, dd, J=9.7, 3.3 Hz), 3.66(2H, s), 3.90–4.02 (2H,m), 4.02–4.17(1H, m), 4.49(1H, d, J=12.2 Hz), 4.54(1H, d, J=12.2 Hz),4.70(1H, d, J=8.7 Hz), 6.64(1H, s), 7.10–7.40(9H, m).

EXAMPLE 82N-[(S)-1-Benzylcarbamoyl-2-phenylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.70–1.80(2H, m), 1.90–2.12(2H, m),3.00–3.20(2H, m), 3.64(2H, s), 3.83–4.00(2H, m), 4.30(1H, dd, J=15.0,5.7 Hz), 4.39(1H, dd, J=15.0, 5.7 Hz), 4.58(1H, dd, J=14.5, 7.5 Hz),5.37(1H, d, J=7.5 Hz), 6.31(1H, br s), 6.73(1H, br s), 7.08(2H, dd,J=7.5, 2.4 Hz), 7.13–7.37(12H, m).

EXAMPLE 83N-[(S)-1-Benzyl-2-(benzylamino)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.60–1.85(2H, m), 1.93–2.14(2H, m),2.68(2H, d, J=5.4 Hz), 2.77(1H, dd, J=13.5, 7.5 Hz), 2.97(1H, dd,J=13.5, 5.4 Hz), 3.02–3.18(2H, m), 3.65(2H, s), 3.75(2H, s), 3.82–4.04(2H, m), 4.07–4.20(1H, m), 5.00(1H, d, J=6.9 Hz), 6.79(1H, br s),7.10–7.36(14H, m).

EXAMPLE 84 Preparation ofN-(2-indanyl)-1-methanesulfonyl-spiro[indoline-3,4′-piperidine]-1′-carboxamide

1-Methanesulfonylspiro[indoline-3,4′-piperidine]hydrochloride (60 mg)and 10M aqueous sodium hydroxide (33 μL) were added to a solution ofphenyl N-(2-indanyl)carbamate (50 mg) in dimethyl sulfoxide (2 mL), andthe mixture was stirred at room temperature for one hour. The reactionmixture was poured into water, and extracted with ethyl acetate. Theorganic layer was dried over anhydrous magnesium sulfate andconcentrated. The residue was washed with ethyl acetate to give thetitle compound (65 mg) as a colorless crystal.

¹H-NMR(300 MHz, CDCl₃, δppm):1.72(2H, d, J=13.9 Hz), 1.83–1.95(2H, m),2.81–2.98(4H, m), 2.91(3H, s), 3.37(2H, dd, J=16.4, 6.4 Hz), 3.84 (2H,s), 3.95(2H, d, J=13.5 Hz), 4.69(2H, br s), 7.06–7.28(7H, m), 7.40(1H,d, J=8.4 Hz).

Compounds of Examples 85 to 88 were obtained by following the sameprocedure as in Example 84, except that phenyl N-(2-indanyl)carbamateand 1-methanesulfonylspiro[indoline-3,4′-piperidine]hydrochloride usedin Example 84 were replaced with the corresponding starting materials ofeach desired compound.

EXAMPLE 851-Methanesulfonyl-N-phenethylspiro[indoline-3,4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.61–1.72(2H, m), 1.79–1.89(2H, m),2.83–2.96(4H, m), 2.86(3H, s), 3.83(2H, s), 3.85–3.94(2H, m), 4.49 (1H,br s), 7.04–7.41(9H, m).

EXAMPLE 861-Methanesulfonyl-N-(3-phenylpropyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.70–1.77(2H, m), 1.86–2.02(2H, m),2.71(2H, t, J=7.4 Hz), 2.88–2.99(2H, m), 2.92(3H, s), 3.33(2H, t, J=7.0Hz), 3.74–3.82(2H, m), 3.84(2H, s), 7.08(1H, t, J=7.4 Hz), 7.15–7.32(8H,m), 7.40(1H, d, J=7.7 Hz).

EXAMPLE 871-Methanesulfonyl-N-(4-phenylbutyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.54–2.00(8H, m), 2.66(2H, t, J=7.3 Hz),2.92(3H, s), 2.93–3.04(2H, m), 3.29(2H, t, J=7.0 Hz), 3.85(2H, s),3.86–3.94(2H, m), 7.07–7.11(1H, m), 7.15–7.31(8H, m), 7.38–7.42(1H, m).

EXAMPLE 88N-(4-Bromophenethyl)-1-methanesulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, DMSO-d₆, δppm):1.55–1.70(4H, m), 2.73(2H, t, J=7.1 Hz),2.78–2.88(2H, m), 3.04(3H, s), 3.22–3.32(2H, m), 3.87(2H, s), 3.91(2H,brd, J=13.2 Hz), 7.06(1H, t, J=7.2 Hz), 7.18–7.29(5H, m), 7.48(2H, d,J=8.2 Hz).

EXAMPLE 89 Preparation ofN-(3,4-dimethoxyphenethyl)-1-methane-sulfonylspiro[indoline-3,4′-piperidine]-1′-carboxamide

2-(4-Formyl-3-methoxyphenoxy)ethyl polystyrene resin (500 mg), 1% aceticacid-dimethylformamide (10 mL), 2-(3,4-dimethoxyphenyl)ethylamine (236μL) and sodium triacetoxyborohydride (590 mg) were successively addedinto a 75 mL-reservoir equipped with a frit. The mixture was stirred atroom temperature overnight and then filtered. The remaining resin waswashed successively with dimethylformamide, methanol and methylenechloride (10 mL each), and dried under reduced pressure to give2-[4-[2-(3,4-dimethoxyphenyl)ethyl]amino-methyl-3-methoxyphenoxy]ethylpolystyrene resin. Then, the resin (50 mg) obtained above, methylenechloride (5 mL), triphosgene (22 mg) and triethylamine (38 μL) wereadded to a 15 mL-reservoir equipped with a frit. The mixture was stirredat room temperature for 6 hours and then filtered. The remaining resinwas washed with methylene chloride, and methylene chloride (5 mL),1-methanesulfonylspiro(indoline-3,4′-piperidine) hydrochloride (22 mg)and triethylamine (77 μL) were added thereto. The mixture was stirred atroom temperature overnight and then filtered. The resin thus obtainedwas washed successively with dimethylformamide, methanol and methylenechloride (10 mL each), and stirred in 50% trifluoroacetic acid-methylenechloride solution for one hour to give a crude product. The product waspurified by chromatography on silica gel to give the title compound (7mg).

¹H-NMR(300 MHz, CDCl₃, δppm):1.65–1.75(2H, m), 1.78–1.93(2H, m),2.80(2H, t, J=6.9 Hz), 2.83–2.98(2H, m), 2.92(3H, s), 3.50(1H, t, J=6.5Hz), 3.52(1H, t, J=6,5 Hz), 3.83(2H, s), 3.86(3H, s), 3.88(3H, s),3.80–3.95(2H, m), 4.51(1H, t), 6.71–6.78(2H, m), 6.79–6.84(1H, m),7.03–7.15(2H, m), 7.20–7.28(1H, m), 7.40(1H, d, J=1.8 Hz).

Compounds of Examples 90 to 95 were obtained by following the sameprocedure as in Example 89, except that2-(3,4-dimethoxyphenyl)ethylamine and1-methanesulfonylspiro[indoline-3,4′-piperidine]hydrochloride used inExample 89 were replaced with the corresponding starting materials ofeach desired compound.

EXAMPLE 901-Methanesulfonyl-N-(3-methoxyphenethyl)spiro[indoline-3,4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.64–1.75(2H, br d, J=13.2 Hz), 1.87 (2H,dt, J=13.2,4.2 Hz), 2.83(2H, t, J=6.5 Hz), 2.85–2.97(2H, m), 2.91(3H,s), 3.51(1H, t, J=6.5 Hz), 3.53(1H, t, J=6.5 Hz), 3.79(3H, s), 3.83(2H,s), 3.84–3.95(2H, br d, J=13.5 Hz), 4.48(1H, t), 6.75–6.81(3H, m),7.07(1H, t, J=7.4 Hz), 7.14(1H, dd, J=7.4, 1.7 Hz), 7.18–7.30(2H, m).

EXAMPLE 91N-(4-Dimethylamino-2-methoxyphenethyl)-1-methanesulfonyl-spiro[indoline-3,4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.65–1.78(2H, m), 2.76(2H, t, J=6.4 Hz),2.91(3H, s), 2.93(6H, s), 2.80–3.00(2H, m), 3.42(1H, t, J=6.4 Hz),3.44(1H, t, J=6.4 Hz), 3.83(5H, s), 3.85–3.97(2H, m), 4.86–4.95(1H, m),6.27(1H, d, J=2.3 Hz), 6.31(1H, dd, J=8.4, 2.3 Hz), 6.95–7.20(4H, m),7.20–7.30(2H, m), 7.39(1H, d, J=6.0 Hz).

EXAMPLE 92N-[(S)-1-Benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.71(2H, br d, J=14.3 Hz), 1.91–2.12 (2H,m), 2.82–3.08(2H, m), 3.30(1H, dd, J=14.4, 5.0 Hz), 3.38(1H, dd, J=14.4,5.0 Hz), 3.63(2H, s), 3.85(2H, br d, J=14.3 Hz), 4.91 (1H, dt, J=8.0,5.0 Hz), 5.01(1H, d, J=8.0 Hz), 5.14(1H, d, J=11.9 Hz), 5.22(1H, d,J=11.9 Hz), 6.34(1H, br s), 6.65(1H, s), 7.09(1H, t, J=6.9 Hz),7.12–7.40(11H, m), 7.55(1H, d, J=8.9 Hz), 7.98(1H, br s).

EXAMPLE 93N-[(R)-1-Benzyloxycarbonyl-2-(3-indolyl)ethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.71(2H, br d, J=14.3 Hz), 1.91–2.12 (2H,m), 2.82–3.08(2H, m), 3.30(1H, dd, J=14.4, 5.0 Hz), 3.38(1H, dd, J=14.4,5.0 Hz), 3.63(2H, s), 3.85(2H, brd, J=14.3 Hz), 4.91(1H, dt, J=8.0, 5.0Hz), 5.01(1H, d, J=8.0 Hz), 5.14(1H, d, J=11.9 Hz), 5.22 (1H, d, J=11.9Hz), 6.34(1H, br s), 6.65(1H, s), 7.09(1H, t, J=6.9 Hz), 7.12–7.40(11H,m), 7.55(1H, d, J=8.9 Hz), 7.98(1H, br s).

EXAMPLE 94N-[(S)-1-Benzyloxycarbonyl-2-cyclohexylethyl]-3,4-dihydro-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):0.82–1.00(2H, m), 1.05–1.41(5H, m),1.46–1.81(6H, m), 1.82(2H, br d, J=12.1 Hz), 2.05–2.10(2H, m),3.05–3.22(2H, m), 3.66(2H, s), 4.03(2H, br t, J=12.1 Hz), 4.60(1H, dt,J=8.3, 5.6 Hz), 4.93(1H, d, J=8.3 Hz), 5.11(1H, d, J=12.4 Hz), 5.24(1H,d, J=12.4 Hz), 6.70(1H, br s), 7.12–7.42(9H, m).

EXAMPLE 953,4-Dihydro-N-(3-methoxyphenethyl)-3-oxospiro[isoquinoline-1(2H),4′-piperidine]-1′-carboxamide

¹H-NMR(300 MHz, CDCl₃, δppm):1.75–1.85(2H, m), 2.02–2.16(2H, m),2.83(2H, t, J=6.8 Hz), 3.02–3.15(2H, m), 3.52(1H, t, J=6.8 Hz), 3.54(1H, t, J=6.8 Hz), 3.66(2H, s), 3.80(3H, s), 3.85–3.98(2H, m),4.47–4.56(1H, m), 6.52(1H, s), 6.72–6.82(3H, m), 7.15–7.32(5H, m).

Industrial Applicability

Compounds of the present invention have NPY antagonistic actions,therefore they are useful as agents for the treatment of variousdiseases related to NPY, for example, cardiovascular disorders such ashypertension, nephropathy, heart disease, vasospasm, arteriosclerosis,etc., central nervous system disorders such as bulimia, depression,anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal,circadian rhythm disorders, schizophrenia, etc., metabolic diseases suchas obesity, diabetes, hormone abnormality, hypercholesterolemia,hyperlipidemia, etc., sexual and reproductive dysfunctions,gastro-intestinal disorders such as gastro-intestinal motility disorder,respiratory disorders, inflammatory diseases or glaucoma.

1. A compound of the formula (I-d):

wherein A is a group selected from formula (A′-1):

which is optionally substituted by a substituent selected from the groupconsisting of oxo, amino, lower alkylamino, di-lower alkylamino,hydroxy, lower alkoxy, lower alkoxycarbonyl, lower alkylene, aryl,heteroaryl and —R^(a); Ar¹ is aryl which is optionally substituted by asubstituent selected from the group consisting of halogen, nitro, oxo,lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-lower alkyl,lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino,di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl and loweralkoxycarbonyl; R^(a) is lower alkyl which is optionally substituted bya substituent selected from the group consisting of amino, loweralkylamino, di-lower alkylamino and hydroxy, and cyclo-lower alkyl, aryland heteroaryl, the last three groups being optionally substituted byfluorine; R⁰ is hydrogen; T, U, V and W are independently methine ornitrogen atom, said methine being optionally substituted by asubstituent selected from the group consisting of halogen, lower alkyl,hydroxy and lower alkoxy, and at least two of T, U, V and W are saidmethine group, or a salt or ester of a carboxyl group thereof when thecompound has carboxyl group.
 2. The compound as claimed in claim 1,wherein all of T, U, V and W are unsubstituted methine.
 3. The compoundas claimed in claim 1, wherein aryl as Ar¹ is phenyl.
 4. The compound asclaimed in claim 1, wherein Ar¹ is aryl which is optionally substitutedby a substituent selected from the group consisting of halogen, nitro,oxo, lower alkyl, halo-lower alkyl, hydroxy-lower alkyl, cyclo-loweralkyl, lower alkenyl, lower alkoxy, halo-lower alkoxy, lower alkylamino,di-lower alkylamino, lower alkylthio, carboxyl, lower alkanoyl and loweralkoxycarbonyl.
 5. The compound as claimed in claim 1, selected from thegroup consisting of:trans-3′-oxo-N-(trans-4-phenylcyclohexyl)spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[(3S)-1-(4-fluorophenyl)-3-pyrrolidinyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[1-(4-fluorophenyl)-4-piperidyl]-3′-oxospiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamidetrans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[5-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[1-(3-fluorophenyl)-4-piperidyl]-3-oxospiro[7-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3′-oxo-N-[(3S)-5-oxo-1-phenyl-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-N-[(3S)-1-(2-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[(3S)-1-(3-fluorophenyl)-3-pyrrolidinyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[5-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3-oxo-N-(trans-4-phenylcyclohexyl)spiro[7-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3-oxo-N-[(3S)-1-phenyl-3-pyrrolidinyl]spiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3-oxo-N-[(3S)-1-(3-trifluoromethylphenyl)-3-pyrrolidinyl]spiro[6-aza-isobenzofuran-1(3H),1′-cyclo-hexane]-4′-carboxamide,trans-N-[trans-4-(4-fluorophenyl)cyclohexyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxo-spiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[trans-4-(3-fluorophenyl)cyclohexyl]-3-oxo-spiro[7-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[(3S)-1-(3,5-difluorophenyl)-3-pyrrolidinyl-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[3-(3-fluorophenyl)-tetrahydropyran-6-yl]-3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[trans-4-(2-fluorophenyl)cyclohexyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[1-(3-trifluoromethylphenyl)-4-piperidyl]3-oxo-spiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-N-[1-(2-fluorophenyl)-4-piperidyl]-3-oxospiro[6-aza-isobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3′-oxo-N-[5-oxo-1-(2-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-3′-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-3-oxo-N-[5-oxo-1-(3-fluorophenyl)-3-pyrrolidinyl]spiro[6-azaisobenzofuran-1(3H),1′-cyclo-hexane]-4′-carboxamide,trans-N-[trans-4-(3-trifluoromethylphenyl)cyclohexyl]3-oxospiro[6-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide,trans-3′-oxo-N-[2-oxo-1-phenyl-4-piperidyl]spiro[cyclo-hexane-1,1′(3′H)-isobenzofuran]-4-carboxamide,trans-3′-oxo-N-[2-oxo-1-(3-fluorophenyl)-4-piperidyl]spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide.6. A composition comprising a compound according to claim 1 togetherwith a pharmaceutically acceptable additive.
 7. The compound or saltthereof of claim 1, wherein the compound istrans-3′-oxo-N-(trans-4-phenylcyclohexyl)-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide.8. The compound or salt thereof of claim 1, wherein the compound istrans-N-[1-(2-fluorophenyl)-4-piperidyl]-3′-oxo-spiro[cyclohexane-1,1′(3′H)-isobenzofuran]-4-carboxamide.9. The compound or salt thereof of claim 1, wherein the compound istrans-N-[1-(3,5-difluorophenyl)-4-piperidyl]-3-oxospiro[4-azaisobenzofuran-1(3H),1′-cyclohexane]-4′-carboxamide.